Compounds > mf 438
Page last updated: 2024-11-12

mf 438

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Description

MF 438: inhibits stearoyl-CoA desaturase 1; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID16042458
CHEMBL ID594902
SCHEMBL ID4265051
MeSH IDM0545626

Synonyms (24)

Synonym
CHEMBL594902 ,
mf-438
2-methyl-5-(6-(4-(2-(trifluoromethyl)phenoxy)piperidin-1-yl)pyridazin-3-yl)-1,3,4-thiadiazole
bdbm50305768
S6842
3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-{4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl}pyridazine
921605-87-0
HI3FN320OX ,
pyridazine, 3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-(4-(2-(trifluoromethyl)phenoxy)-1-piperidinyl)-
unii-hi3fn320ox
SCHEMBL4265051
mf 438
E73480
HY-15822
BS-45413
CS-0009306
Q27279943
EX-A4365
3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]-1-piperidinyl]pyridazine
AC-36563
SB41043
2-methyl-5-[6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazin-3-yl]-1,3,4-thiadiazole
3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-(4-(2-(trifluoromethyl)phenoxy)-1-piperidinyl)pyridazine
AKOS040742136

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
"It has been demonstrated that once-a-day dosing of systemically-distributed SCD inhibitors leads to adverse events in eye and skin."( Conversion of systemically-distributed triazole-based stearoyl-CoA desaturase (SCD) uHTS hits into liver-targeted SCD inhibitors.
Falgueyret, JP; Girardin, M; Guay, J; Guiral, S; Huang, Z; Leclerc, JP; Li, CS; Oballa, R; Ramtohul, YK; Skorey, K; Tawa, P; Wang, H; Zhang, L, 2011)		0.37
[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)
Stearoyl-CoA desaturaseHomo sapiens (human)IC50 (µMol)0.02100.00100.35661.0700AID692198
Acyl-CoA (8-3)-desaturaseHomo sapiens (human)IC50 (µMol)100,000.00000.01100.01100.0110AID692205
Acyl-CoA desaturase 1Rattus norvegicus (Norway rat)IC50 (µMol)0.05370.00040.15941.7100AID627999; AID692197; AID692199
Acyl-CoA Rattus norvegicus (Norway rat)IC50 (µMol)100,000.00000.00840.00840.0084AID692204
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (16)

Processvia Protein(s)Taxonomy
unsaturated fatty acid biosynthetic processStearoyl-CoA desaturaseHomo sapiens (human)
positive regulation of cold-induced thermogenesisStearoyl-CoA desaturaseHomo sapiens (human)
monounsaturated fatty acid biosynthetic processStearoyl-CoA desaturaseHomo sapiens (human)
response to fatty acidStearoyl-CoA desaturaseHomo sapiens (human)
unsaturated fatty acid biosynthetic processAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
long-chain fatty acid biosynthetic processAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
regulation of DNA-templated transcriptionAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
unsaturated fatty acid biosynthetic processAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
cell-cell signalingAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
phospholipid biosynthetic processAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
cellular response to starvationAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
alpha-linolenic acid metabolic processAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
linoleic acid metabolic processAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
regulation of cell differentiationAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
icosanoid biosynthetic processAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
lipid metabolic processAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
arachidonic acid metabolite production involved in inflammatory responseAcyl-CoA 6-desaturaseHomo sapiens (human)
unsaturated fatty acid biosynthetic processAcyl-CoA 6-desaturaseHomo sapiens (human)
alpha-linolenic acid metabolic processAcyl-CoA 6-desaturaseHomo sapiens (human)
linoleic acid metabolic processAcyl-CoA 6-desaturaseHomo sapiens (human)
positive regulation of cellular response to oxidative stressAcyl-CoA 6-desaturaseHomo sapiens (human)
lipid metabolic processAcyl-CoA 6-desaturaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
stearoyl-CoA 9-desaturase activityStearoyl-CoA desaturaseHomo sapiens (human)
iron ion bindingStearoyl-CoA desaturaseHomo sapiens (human)
protein bindingStearoyl-CoA desaturaseHomo sapiens (human)
oxidoreductase activityStearoyl-CoA desaturaseHomo sapiens (human)
palmitoyl-CoA 9-desaturase activityStearoyl-CoA desaturaseHomo sapiens (human)
C-5 sterol desaturase activityAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
linoleoyl-CoA desaturase activityAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
oxidoreductase activityAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
omega-6 fatty acid desaturase activityAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
acyl-CoA delta5-desaturase activityAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
oxidoreductase activity, acting on paired donors, with oxidation of a pair of donors resulting in the reduction of molecular oxygen to two molecules of waterAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
stearoyl-CoA 9-desaturase activityAcyl-CoA 6-desaturaseHomo sapiens (human)
linoleoyl-CoA desaturase activityAcyl-CoA 6-desaturaseHomo sapiens (human)
oxidoreductase activity, acting on paired donors, with oxidation of a pair of donors resulting in the reduction of molecular oxygen to two molecules of waterAcyl-CoA 6-desaturaseHomo sapiens (human)
omega-6 fatty acid desaturase activityAcyl-CoA 6-desaturase Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
nucleolusStearoyl-CoA desaturaseHomo sapiens (human)
endoplasmic reticulumStearoyl-CoA desaturaseHomo sapiens (human)
endoplasmic reticulum membraneStearoyl-CoA desaturaseHomo sapiens (human)
membraneStearoyl-CoA desaturaseHomo sapiens (human)
endoplasmic reticulum membraneStearoyl-CoA desaturaseHomo sapiens (human)
mitochondrionAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
endoplasmic reticulum membraneAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
membraneAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
intracellular membrane-bounded organelleAcyl-CoA (8-3)-desaturaseHomo sapiens (human)
endoplasmic reticulum membraneAcyl-CoA 6-desaturaseHomo sapiens (human)
plasma membraneAcyl-CoA 6-desaturaseHomo sapiens (human)
membraneAcyl-CoA 6-desaturaseHomo sapiens (human)
endoplasmic reticulum membraneAcyl-CoA 6-desaturase Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (46)

Assay IDTitleYearJournalArticle
AID692434Antidiabetic activity in diet-induced obese C57BL6 mouse assessed as reduction in glucose AUC at 1 to 15 mg/kg, po administered 1 hr before oral glucose administration measured 2 hrs thereafter2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692458Toxicity in diet-induced obese C57BL6 mouse assessed as reduction in food intake at 1 to 5 mg/kg, po QD2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID453701Inhibition of stearoyl-CoA dehydrogenase in high-carbohydrate diet-fed mouse liver dosed orally assessed as conversion of [14C]stearic acid to [14C]oleic acid2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).
AID692467Inhibition of SCD activity in harderian gland of diet-induced obese C57BL6 mouse assessed as reduction in desaturation induces at 5 mg/kg, po QD2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692432Antidiabetic activity in diet-induced obese C57BL6 mouse assessed as reduction in glucose AUC at 1 to 3 mg/kg, po administered 1 hr before oral glucose administration measured 2 hrs thereafter2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692199Inhibition of SCD-1 activity in Sprague-Dawley rat Hepatocytes expressing organic anion transporting polypeptides assessed as reduction in [I-14C] stearoyl CoA desaturation by scintillation counting2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692431Antidiabetic activity in po dosed diet-induced obese fasted C57BL6 mouse assessed as increase in glucose clearance administered 1 hr before glucose challenge measured 12 hrs thereafter by OGTT2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692455Antidiabetic activity in po dosed diet-induced obese C57BL6 mouse assessed as reduction in body weight gain2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692442AUC in plasma of fasted C57BL6 mouse at 2 mg/kg, iv and 10 mg/kg, po by LC-MS-MS analysis2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692460Toxicity in diet-induced obese C57BL6 mouse assessed as adverse effect in skin at 1 to 5 mg/kg, po QD2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692483Inhibition of SCD activity in liver of diet-induced obese C57BL6 mouse assessed as reduction in desaturation induces at 30 mg/kg, po BID2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692200Ratio IC50 for SCD-1 activity in organic anion transporting polypeptides-deficient human HepG2 cells to IC50 for SCD-1 activity in Sprague-Dawley rat Hepatocytes expressing organic anion transporting polypeptides2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID453718Toxicity in DIO mouse assessed as partial eye closure at 5 mg/kg qd for 1 week2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).
AID692466Inhibition of SCD activity in liver of diet-induced obese C57BL6 mouse assessed as reduction in desaturation induces at 5 mg/kg, po QD2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692206Inhibition of rat delta-6 desaturase activity expressed in human HEpG2 cells2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692433Antidiabetic activity in diet-induced obese C57BL6 mouse assessed as reduction in glucose AUC at 1 to 10 mg/kg, po administered 1 hr before oral glucose administration measured 2 hrs thereafter2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID453715Inhibition of CYP2D6 up to 30 uM2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).
AID453710Oral bioavailability in rat2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).
AID453713Half life in rat2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).
AID692438Clearance in fasted C57BL6 mouse at 2 mg/kg, iv and 10 mg/kg, po by LC-MS-MS analysis2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID453717Toxicity in DIO mouse assessed as alopecia at 5 mg/kg qd for 1 week2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).
AID692204Inhibition of rat delta-5 desaturase activity expressed in human HEpG2 cells2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID453712Half life in mouse2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).
AID453702Inhibition of SCD1 in rat liver microsomes2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).
AID692452Antidiabetic activity in diet-induced obese C57BL6 mouse assessed as reduction in body weight gain at 5 mg/kg, po QD2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692228Ratio drug uptake in liver to harderian gland of C57BL6 mouse at 10 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692469Drug level in liver of diet-induced obese C57BL6 mouse at 5 mg/kg, po QD2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692205Inhibition of human delta-5 desaturase activity expressed in human HEpG2 cells2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692451Antidiabetic activity in diet-induced obese C57BL6 mouse assessed as reduction in body weight gain at 1 mg/kg, po QD2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692207Inhibition of human delta6 desaturase activity expressed in human HEpG2 cells2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692461Toxicity in diet-induced obese C57BL6 mouse assessed as adverse effect in eye at 1 to 5 mg/kg, po QD2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692471Drug level in skin of diet-induced obese C57BL6 mouse at 5 mg/kg, po QD2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID453711Oral bioavailability in mouse2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).
AID692197Inhibition of SCD-1 activity in Sprague-Dawley rat microsome assessed as reduction in [I-14C] stearoyl CoA desaturation by scintillation counting2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692468Inhibition of SCD activity in skin of diet-induced obese C57BL6 mouse assessed as reduction in desaturation induces at 5 mg/kg, po QD2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692232Ratio drug uptake in liver to plasma of C57BL6 mouse at 10 mg/kg, po measured 6 hrs post dose2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID453714Inhibition of CYP3A4 up to 30 uM2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).
AID692198Inhibition of SCD-1 activity in organic anion transporting polypeptides-deficient human HepG2 cells assessed as reduction in [I-14C] stearoyl CoA desaturation by scintillation counting2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID453716Toxicity in high-carbohydrate diet-fed chronic po dosed mouse2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).
AID627999Inhibition of rat SCD by rat microsomal assay2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Conversion of systemically-distributed triazole-based stearoyl-CoA desaturase (SCD) uHTS hits into liver-targeted SCD inhibitors.
AID692450Oral bioavailability in C57BL6 mouse at 10 mg/kg QD2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692443Cmin in liver of fasted C57BL6 mouse at 5 mg/kg, po QD by LC-MS-MS analysis2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692440Half life in fasted C57BL6 mouse at 2 mg/kg, iv and 10 mg/kg, po by LC-MS-MS analysis2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692470Drug level in harderian gland of diet-induced obese C57BL6 mouse at 5 mg/kg, po QD2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692441Cmax in plasma of fasted C57BL6 mouse at 2 mg/kg, iv and 10 mg/kg, po by LC-MS-MS analysis2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
AID692439Volume of distribution in fasted C57BL6 mouse at 2 mg/kg, iv and 10 mg/kg, po by LC-MS-MS analysis2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (83.33)24.3611
2020's1 (16.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 23.16

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 Index23.16 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index5.21 (4.65)
Search Engine Demand Index19.78 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.16)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
hydrochloric acid
Hydrochloric Acid: A strong corrosive acid that is commonly used as a laboratory reagent. It is formed by dissolving hydrogen chloride in water. GASTRIC ACID is the hydrochloric acid component of GASTRIC JUICE.. hydrogen chloride : A mononuclear parent hydride consisting of covalently bonded hydrogen and chlorine atoms.		2.2110chlorine molecular entity;
gas molecular entity;
hydrogen halide;
mononuclear parent hydride		mouse metabolite
hydroxylamine
amino alcohol : An alcohol containing an amino functional group in addition to the alcohol-defining hydroxy group.		2.2110hydroxylaminesalgal metabolite;
bacterial xenobiotic metabolite;
EC 1.1.3.13 (alcohol oxidase) inhibitor;
EC 4.2.1.22 (cystathionine beta-synthase) inhibitor;
EC 4.3.1.10 (serine-sulfate ammonia-lyase) inhibitor;
nitric oxide donor;
nucleophilic reagent
am 251
AM 251: an analog of SR141716A; structure given in first source. AM-251 : A carbohydrazide obtained by formal condensation of the carboxy group of 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid with the amino group of 1-aminopiperidine. An antagonist at the CB1 cannabinoid receptor.		2.0610amidopiperidine;
carbohydrazide;
dichlorobenzene;
organoiodine compound;
pyrazoles		antidepressant;
antineoplastic agent;
apoptosis inducer;
CB1 receptor antagonist
pyridazine
pyridazine: structure given in first source		2.0510diazine;
pyridazines
sodium hydroxide
Sodium Hydroxide: A highly caustic substance that is used to neutralize acids and make sodium salts. (From Merck Index, 11th ed)		2.2110alkali metal hydroxide
alpha-synuclein
alpha-Synuclein: A synuclein that is a major component of LEWY BODIES and plays a role in SYNUCLEINOPATHIES, neurodegeneration and neuroprotection.		2.2510
mk 8245
[no description available]		2.0610
ConditionIndicatedRelationship StrengthStudiesTrials
Cortical Lewy Body Disease
[description not available]		02.2510
Idiopathic Parkinson Disease
[description not available]		02.2510
Neuroblastoma
A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51)		02.2510
Parkinson Disease
A progressive, degenerative neurologic disease characterized by a TREMOR that is maximal at rest, retropulsion (i.e. a tendency to fall backwards), rigidity, stooped posture, slowness of voluntary movements, and a masklike facial expression. Pathologic features include loss of melanin containing neurons in the substantia nigra and other pigmented nuclei of the brainstem. LEWY BODIES are present in the substantia nigra and locus coeruleus but may also be found in a related condition (LEWY BODY DISEASE, DIFFUSE) characterized by dementia in combination with varying degrees of parkinsonism. (Adams et al., Principles of Neurology, 6th ed, p1059, pp1067-75)		02.2510
Lewy Body Disease
A neurodegenerative disease characterized by dementia, mild parkinsonism, and fluctuations in attention and alertness. The neuropsychiatric manifestations tend to precede the onset of bradykinesia, MUSCLE RIGIDITY, and other extrapyramidal signs. DELUSIONS and visual HALLUCINATIONS are relatively frequent in this condition. Histologic examination reveals LEWY BODIES in the CEREBRAL CORTEX and BRAIN STEM. SENILE PLAQUES and other pathologic features characteristic of ALZHEIMER DISEASE may also be present. (From Neurology 1997;48:376-380; Neurology 1996;47:1113-1124)		02.2510
Adenocarcinoma, Basal Cell
[description not available]		02.1510
Carcinoma, Non-Small Cell Lung
[description not available]		02.1510
Carcinoma, Epidermoid
[description not available]		02.1510
Cancer of Lung
[description not available]		02.1510
Adenocarcinoma
A malignant epithelial tumor with a glandular organization.		02.1510
Carcinoma, Non-Small-Cell Lung
A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.		02.1510
Carcinoma, Squamous Cell
A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)		02.1510
Lung Neoplasms
Tumors or cancer of the LUNG.		02.1510