Page last updated: 2024-11-12

dirlotapide

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Description

dirlotapide: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9917862
CHEMBL ID410414
SCHEMBL ID37781
MeSH IDM0511637

Synonyms (38)

Synonym
cp 742033
dirlotapide
481658-94-0
dirlotapide (usan/inn)
slentrol [veterinary] (tn)
D03867
CHEMBL410414 ,
slentrol
cp-742,033
cp-742033
bdbm50204367
unii-578h0rmp25
578h0rmp25 ,
n-((1s)-2-(benzylmethylamino)-2-oxo-1-phenylethyl)-1-methyl-5-(((4'-(trifluoromethyl)biphenyl-2-yl)carbonyl)amino)-1h-indole-2-carboxamide
dirlotapide [usan:inn]
5-((4'-trifluoromethyl-biphenyl-2-carbonyl)-amino)-1h-indole-2-carboxylic acid benzylmethyl carbamoylamide
1h-indole-2-carboxamide, 1-methyl-n-((1s)-2-(methyl(phenylmethyl)amino)-2-oxo-1-phenylethyl)-5-(((4'-(trifluoromethyl)(1,1'-biphenyl)-2-yl)carbonyl)amino)-
dirlotapide [usan]
dirlotapide [inn]
dirlotapide [green book]
dirlotapide [ema epar veterinary]
dirlotapide [mi]
SCHEMBL37781
(s)-n-{2-[benzyl(methyl)amino]-2-oxo-1-phenylethyl}-1-methyl-5-[4'-(trifluoromethyl)[1,1'-biphenyl]-2-carboxamido]-1h-indole-2-carboxamide
HY-U00070
CS-6779
DTXSID00897432 ,
Q5280905
DB11399
(s)-n-(2-(benzyl(methyl)amino)-2-oxo-1-phenylethyl)-1-methyl-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-2-carboxamido)-1h-indole-2-carboxamide
MS-31064
n-[(1s)-2-[benzyl(methyl)amino]-2-oxo-1-phenylethyl]-1-methyl-5-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]indole-2-carboxamide
dirlotapidum
dtxcid501326773
slentrol (veterinary)
dirlotapida
dirlotapide (ema epar veterinary)
AKOS040741569

Research Excerpts

Overview

Dirlotapide is a microsomal triglyceride transfer protein (MTP) inhibitor. It is intended for the treatment and management of obesity in dogs.

ExcerptReferenceRelevance
"Dirlotapide is a microsomal triglyceride transfer protein (MTP) inhibitor developed specifically for canine weight reduction. "( Dirlotapide: a review of its properties and role in the management of obesity in dogs.
Gossellin, J; Sunderland, SJ; Wren, JA, 2007
)
3.23
"Dirlotapide is a novel microsomal triglyceride transfer protein inhibitor intended for the treatment and management of obesity in dogs. "( Biologic activity of dirlotapide, a novel microsomal triglyceride transfer protein inhibitor, for weight loss in obese dogs.
Campbell, SL; Hickman, MA; King, VL; Wren, JA, 2007
)
2.1

Treatment

Dirlotapide-treated dogs showed mean weight loss of 15.9% (study A) and 14.0% ( study B) by the end of weight loss phase (up to day 196). For dirlotapside- treated dogs, mean weight lost by day 112 was 11.8-14.0%. For placebo, mean Weight Loss by Day 112 was 3.0-3.9%.

ExcerptReferenceRelevance
"Dirlotapide-treated dogs showed mean weight loss of 15.9% (study A) and 14.0% (study B) by the end of weight loss phase (up to day 196)."( An evaluation of dirlotapide to reduce body weight of client-owned dogs in two placebo-controlled clinical studies in Europe.
Eagleson, JS; Gossellin, J; McKelvie, J; Rowan, TG; Sherington, J; Sunderland, SJ; Wren, JA, 2007
)
1.4
"For dirlotapide-treated dogs, mean weight loss by day 112 was 11.8-14.0% compared with 3.0-3.9% for placebo (P = 0.0001)."( Efficacy and safety of dirlotapide in the management of obese dogs evaluated in two placebo-controlled, masked clinical studies in North America.
Campbell, SL; Eagleson, JS; Gossellin, J; King, VL; Ramudo, AA; Sunderland, SJ; Wren, JA, 2007
)
1.13

Toxicity

ExcerptReferenceRelevance
" Results were similar for both studies, and no serious adverse events were observed."( The safety of dirlotapide in dogs.
Gossellin, J; Hickman, MA; Kerlin, RL; King, VL; Krautmann, MJ; Schmahai, TJ; Wren, JA, 2007
)
0.7
" Dirlotapide was safe and effective in the reduction and management of body weight in obese dogs."( Efficacy and safety of dirlotapide in the management of obese dogs evaluated in two placebo-controlled, masked clinical studies in North America.
Campbell, SL; Eagleson, JS; Gossellin, J; King, VL; Ramudo, AA; Sunderland, SJ; Wren, JA, 2007
)
1.56

Bioavailability

ExcerptReferenceRelevance
" Oral bioavailability was 22-41%."( Pharmacokinetics of dirlotapide in the dog.
King, VL; Lynch, MP; Merritt, DA, 2007
)
0.66
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)30.00000.00011.774010.0000AID299017
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)30.00000.00011.753610.0000AID299021
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)30.00000.00002.015110.0000AID299020
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)30.00000.00002.800510.0000AID299018
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)30.00000.00002.398310.0000AID299019
Microsomal triglyceride transfer protein large subunitHomo sapiens (human)IC50 (µMol)0.00190.00000.72635.7500AID298875; AID688268; AID688269
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (59)

Processvia Protein(s)Taxonomy
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
lipid metabolic processMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
triglyceride metabolic processMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
circadian rhythmMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
protein secretionMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
phospholipid transportMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
sterol transportMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
triglyceride transportMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
low-density lipoprotein particle remodelingMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
plasma lipoprotein particle assemblyMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
chylomicron assemblyMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
very-low-density lipoprotein particle assemblyMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
lipoprotein transportMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
response to calcium ionMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
establishment of localization in cellMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
intermembrane lipid transferMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
ceramide 1-phosphate transportMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
lipoprotein metabolic processMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
cholesterol homeostasisMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (46)

Processvia Protein(s)Taxonomy
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
lipid transporter activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
protein bindingMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
lipid bindingMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
apolipoprotein bindingMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
protein-containing complex bindingMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
protein heterodimerization activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
phospholipid transfer activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
phosphatidylcholine transfer activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
cholesterol transfer activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
triglyceride transfer activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
ceramide 1-phosphate transfer activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
phosphatidylethanolamine transfer activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
phospholipid transporter activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (14)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
endoplasmic reticulumMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
endoplasmic reticulum lumenMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
Golgi apparatusMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
cytosolMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
brush border membraneMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
microvillus membraneMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
vesicleMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
receptor complexMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
Golgi apparatusMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
endoplasmic reticulumMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
basolateral plasma membraneMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (175)

Assay IDTitleYearJournalArticle
AID417508Inhibition of apoB secretion in human HepG2 cells after 40 hrs by ELISA2009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
Discovery of benzothiazole derivatives as efficacious and enterocyte-specific MTP inhibitors.
AID299009Decrease in food intake in obese Beagle dog at 0.39 mg/kg, po after 3 months2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298973AUC (0 to infinity) in rat at 0.3 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID299007Bioavailability in Beagle dog at 5 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298929Clearance in human liver microsomes2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298881Inhibition of adrenergic a2 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298915Inhibition of mu opioid receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298918Inhibition of tachykinin receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298991Cmax in rat at 30 mg/kg, po after 2.8 hrs2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298896Inhibition of NMDA receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298884Inhibition of AT1 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298992Cmax in rat at 300 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298942Ratio of drug level in blood to plasma in rat2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID299010Decrease in cholesterol level in obese Beagle dog at 0.39 mg/kg, po after 3 months2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688124Antiobesity activity in high fat diet-induced obese Sprague-Dawley rat assessed as reduction of body weight at 30 mg/kg, po qd for 7 days2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID688266Antiobesity activity in high fat diet-induced obese Sprague-Dawley rat assessed as reduction of food intake at 10 mg/kg, po administered daily for 3 days relative to control2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID298875Inhibition of MTP assessed as inhibition of apoB secretion from human HepG2 cells2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298959Volume of distribution at steady state in monkey at 0.5 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298952Plasma clearance in portal cannulated Beagle dog at 1 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298953Plasma clearance in monkey at 0.5 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID299020Inhibition of CYP2D62007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298928Clearance in monkey liver microsomes2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID299017Inhibition of CYP1A22007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298923Intrinsic clearance in dog microsomes2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298922Intrinsic clearance in rat microsomes2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298951Plasma clearance in Beagle dog at 1 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688126Antiobesity activity in high fat diet-induced obese Sprague-Dawley rat assessed as reduction of body weight at 3 mg/kg, po qd for 7 days relative to control2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID298985AUC (0 to infinity) in rat at 3 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298977AUC (0 to infinity) in Beagle dog at 1 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298889Inhibition of dopamine D1 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID299016Permeability from basolateral to apical side of the Caco-2 cell membrane at 10 uM in presence of calcium2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298931Clearance in human hepatocytes2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298887Inhibition of bradykinin B1 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688129Antiobesity activity in high fat diet-induced obese Sprague-Dawley rat assessed as reduction of food intake at 3 mg/kg, po qd for 7 days relative to control2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID688128Antiobesity activity in high fat diet-induced obese Sprague-Dawley rat assessed as reduction of food intake at 10 mg/kg, po qd for 7 days relative to control2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID298936Metabolic stability in human liver microsome at 0.5 uM in presence of 5 uM CYP2D6 inhibitor quinidine2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298924Intrinsic clearance in monkey microsomes2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298914Inhibition of kappa opioid receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298999Tmax in portal cannulated Beagle dog at 1 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298970AUC (0 to t) in Beagle dog at 0.5 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688127Antiobesity activity in high fat diet-induced obese Sprague-Dawley rat assessed as reduction of food intake at 30 mg/kg, po qd for 7 days relative to control2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID298974AUC (0 to infinity) in rat at 1 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298895Inhibition of kainate receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298902Inhibition of 5HT2C receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688123Antiobesity activity in high fat diet-induced obese Sprague-Dawley rat assessed as reduction of triglyceride accumulation in liver at 3 mg/kg, po qd for 7 days relative to control2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID688265Antiobesity activity in high fat diet-induced obese Sprague-Dawley rat assessed as reduction in body weight at 10 mg/kg, po administered daily for 3 days relative to control2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID298949Plasma clearance in rat at 5 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298958Volume of distribution at steady state in Beagle dog at 1 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298976AUC (0 to infinity) in Beagle dog at 0.5 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688122Antiobesity activity in high fat diet-induced obese Sprague-Dawley rat assessed as reduction of triglyceride accumulation in liver at 10 mg/kg, po qd for 7 days relative to control2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID298933Metabolic stability in human liver microsome at 0.5 uM in presence of 1 uM CYP3A4 inhibitor ketoconazole2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298978AUC (0 to infinity) in portal cannulated Beagle dog at 1 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298983Half life in Beagle dog at 0.5 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298946Inhibition of hepatic MTP in mouse assessed as reduction of triglyceride2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298903Inhibition of 5HT3 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688268Inhibition of MTP in human HepG2 cells assessed as unbound drug level causing inhibition of apoB secretion after 40 hrs by ELISA2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID298947Plasma clearance in rat at 0.3 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID299002Bioavailability in rat at 3 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298879Inhibition of adenosine A3 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298962Half life in rat at 5 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID299008Effect on body weight in obese Beagle dog assessed as weight loss at 0.39 mg/kg, po after 3 months relative to control2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298926Clearance in rat liver microsomes2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298908Inhibition of muscarinic M2 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298961Half life in rat at 1 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298917Inhibition of glucocorticoid receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID299018Inhibition of CYP2C92007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298964Half life in Beagle dog at 1 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID299012Permeability from apical to basolateral side of the Caco-2 cell membrane at 1 uM in presence of calcium2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID299015Permeability from basolateral to apical side of the Caco-2 cell membrane at 1 uM in presence of calcium2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298906Inhibition of melanocortin MC4 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298997Tmax in rat at 30 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298930Clearance in rat hepatocytes2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID299014Permeability from apical to basolateral side of the Caco-2 cell membrane at 10 uM in presence of calcium2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298913Inhibition of delta opioid receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298934Metabolic stability in human liver microsome at 0.5 uM in presence of 5 uM CYP2C9 inhibitor sulfaphenazole2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688116AUC in high fat diet-induced obese Sprague-Dawley rat at 30 mg/kg, po qd for 7 days2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID298904Inhibition of 5HT4 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298941Percentage unbound ligand in human blood at 0.2 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688269Inhibition of MTP in human HepG2 cells assessed as inhibition of apoB secretion after 40 hrs by ELISA2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID298920Inhibition of N-type calcium channel at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298954Volume of distribution at steady state in rat at 0.3 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298898Inhibition of histamine H2 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298886Inhibition of central benzodiazepine receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298967AUC (0 to t) in rat at 0.3 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298897Inhibition of histamine H1 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298880Inhibition of adrenergic a1 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298996Tmax in rat at 3 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298900Inhibition of 5HT1A receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688101Antiobesity activity in po dosed high fat diet-induced obese Sprague-Dawley rat assessed as reduction of reduction of triglyceride accumulation in liver administered daily for 3 days2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID298968AUC (0 to t) in rat at 1 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298998Tmax in rat at 300 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID417509Inhibition of MTP from dog liver microsomes by scintillation counting2009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
Discovery of benzothiazole derivatives as efficacious and enterocyte-specific MTP inhibitors.
AID298893Inhibition of GABA receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298979AUC (0 to infinity) in monkey at 0.5 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298994Cmax in Beagle dog at 0.5 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298986AUC (0 to infinity) in male rat at 30 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298907Inhibition of muscarinic M1 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298989AUC (0 to infinity) in Beagle dog at 5 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688125Antiobesity activity in high fat diet-induced obese Sprague-Dawley rat assessed as reduction of body weight at 10 mg/kg, po qd for 7 days relative to control2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID298888Inhibition of bradykinin B2 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298921Inhibition of IKr potassium channel at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298965Half life in portal cannulated Beagle dog at 1 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298956Volume of distribution at steady state in rat at 5 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298935Metabolic stability in human liver microsome at 0.5 uM in presence of 200 uM CYP2C19 inhibitor (S)-mephenytoin2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298944Ratio of drug level in blood to plasma in human2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298963Half life in Beagle dog at 0.5 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298972AUC (0 to t) in monkey at 0.5 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298950Plasma clearance in Beagle dog at 0.5 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298919Inhibition of L-type calcium channel at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298990Cmax in rat at 3 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688264Antiobesity activity in high fat diet-induced obese Sprague-Dawley rat assessed as reduction of triglyceride accumulation in liver at 10 mg/kg, po administered daily for 3 days relative to control2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID299004Bioavailability in rat at 300 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688115AUC in high fat diet-induced obese Sprague-Dawley rat at 10 mg/kg, po qd for 7 days2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID298901Inhibition of 5HT2A receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298938Percentage unbound ligand in rat blood at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298955Volume of distribution at steady state in rat at 1 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688099Antiobesity activity in po dosed high fat diet-induced obese Sprague-Dawley rat assessed as reduction of food intake administered daily for 3 days2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID298932Metabolic stability in human liver microsome at 0.5 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298975AUC (0 to infinity) in rat at 5 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298943Ratio of drug level in blood to plasma in dog2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298916Inhibition of platelet activating factor receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298925Intrinsic clearance in human microsomes2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688100Antiobesity activity in po dosed high fat diet-induced obese Sprague-Dawley rat assessed as reduction of body weight administered daily for 3 days2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID688267Fraction unbound in human HepG2 cells by equilibrium dialysis2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID299001Tmax in Beagle dog at 5 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID299019Inhibition of CYP2C192007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID638992Activity of recombinant CYP3A4 assessed as metabolite formation2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Dirlotapide as a model substrate to refine structure-based drug design strategies on CYP3A4-catalyzed metabolism.
AID298948Plasma clearance in rat at 1 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298980Half life in rat at 3 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298878Inhibition of adenosine A2a receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298971AUC (0 to t) in Beagle dog at 1 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298987AUC (0 to infinity) in portal cannulated Beagle dog at 1 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688111Toxicity in high fat diet-induced obese Sprague-Dawley rat assessed as change in serum ALT level at 3 mg/kg, po qd for 7 days relative to control2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID298911Inhibition of neuronal nicotinic receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298966Half life in monkey at 0.5 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298984Half life in Beagle dog at 5 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298939Percentage unbound ligand in dog blood at 0.2 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298927Clearance in dog liver microsomes2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298890Inhibition of dopamine D2 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298982Half life in portal cannulated Beagle dog at 1 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID299013Permeability from apical to basolateral side of the Caco-2 cell membrane at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298894Inhibition of AMPA receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID299005Bioavailability in portal cannulated Beagle dog at 1 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298981Half life in rat at 30 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298899Inhibition of histamine H3 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298957Volume of distribution at steady state in Beagle dog at 0.5 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID299021Inhibition of CYP3A42007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298876Inhibition of MTP assessed as inhibition of apoB secretion from canine hepatocytes2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298993Cmax in portal cannulated Beagle dog at 1 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688113Toxicity in high fat diet-induced obese Sprague-Dawley rat assessed as change in serum ALT level at 30 mg/kg, po qd for 7 days relative to control2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID298883Inhibition of adrenergic b2 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298909Inhibition of muscarinic M3 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298945Inhibition of intestinal MTP in mouse assessed as inhibition of intestinal fat absorption2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298885Inhibition of AT2 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID299011Increase in fecal fat in obese Beagle dog at 0.39 mg/kg, po after 3 months2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298940Percentage unbound ligand in monkey blood at 0.2 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688121Antiobesity activity in high fat diet-induced obese Sprague-Dawley rat assessed as reduction of triglyceride accumulation in liver at 30 mg/kg, po qd for 7 days relative to control2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID299006Bioavailability in Beagle dog at 0.5 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID299003Bioavailability in rat at 30 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID638991Drug metabolism in human liver microsomes at 20 mM2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Dirlotapide as a model substrate to refine structure-based drug design strategies on CYP3A4-catalyzed metabolism.
AID298969AUC (0 to t) in rat at 5 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298905Inhibition of 5HT7 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298960Half life in rat at 0.3 mg/kg, iv2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298892Inhibition of dopamine D4 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298912Inhibition of muscle nicotinic receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688112Toxicity in high fat diet-induced obese Sprague-Dawley rat assessed as change in serum ALT level at 10 mg/kg, po qd for 7 days relative to control2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID299000Tmax in Beagle dog at 0.5 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298877Inhibition of adenosine A1 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID688114AUC in high fat diet-induced obese Sprague-Dawley rat at 3 mg/kg, po qd for 7 days2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
AID298882Inhibition of adrenergic b1 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298995Cmax in Beagle dog at 5 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298910Inhibition of muscarinic M4 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298988AUC (0 to infinity) in Beagle dog at 0.5 mg/kg, po2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298891Inhibition of dopamine D3 receptor at 1 uM2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
AID298937Metabolic stability in human liver microsome at 0.5 uM in presence of 5 uM CYP1A2 inhibitor furafylline2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (16)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's11 (68.75)29.6817
2010's4 (25.00)24.3611
2020's1 (6.25)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.04

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index29.04 (24.57)
Research Supply Index3.18 (2.92)
Research Growth Index4.43 (4.65)
Search Engine Demand Index53.70 (26.88)
Search Engine Supply Index3.39 (0.95)

This Compound (29.04)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (43.75%)5.53%
Reviews1 (6.25%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (50.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]