Compounds > l 753037
Page last updated: 2024-09-26

l 753037

Description

J 104132: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID186002
CHEMBL ID305576
SCHEMBL ID6439800
MeSH IDM0305530

Synonyms (26)

Synonym
l 753037
j-104132
2-butyl-7-(2-((2s)-2-carboxypropyl)-4-methoxyphenyl)-5-(4-methylenedioxyphenyl)cyclopenteno(1,2-b)pyridine-6-carboxylic
l-753,037
j 104132
PDSP2_001713
(5s,6r,7r)-5-benzo[1,3]dioxol-5-yl-2-butyl-7-[2-((s)-2-carboxy-propyl)-4-methoxy-phenyl]-6,7-dihydro-5h-[1]pyrindine-6-carboxylic acid
bdbm50143784
CHEMBL305576 ,
224448-58-2
5h-cyclopenta(b)pyridine-6-carboxylic acid, 5-(1,3-benzodioxol-5-yl)-2-butyl-7-(2-((2s)-2-carboxypropyl)-4-methoxyphenyl)-6,7-dihydro-, (5s,6r,7r)-
198279-45-7
unii-n71z6m3t0i
5h-cyclopenta(b)pyridine-6-carboxylic acid, 5-(1,3-benzodioxol-5-yl)-2-butyl-7-(2-(2-carboxypropyl)-4-methoxyphenyl)-6,7-dihydro-, (5s-(5alpha,6beta,7alpha(r*)))-
n71z6m3t0i ,
mk-547 parent
DTXSID9047332
SCHEMBL6439800
l-753037
5h-cyclopenta(b)pyridine-6-carboxylic acid, 5-(1,3-benzodioxol-5-yl)-2-butyl-7-(2-(2-carboxypropyl)-4-methoxyphenyl)-6,7-dihydro-, (5s-(5.alpha.,6.beta.,7.alpha.(r*)))-
AKOS030532233
HY-10383
CS-5666
(5s,6r,7r)-5-(benzo[d][1,3]dioxol-5-yl)-2-butyl-7-(2-((s)-2-carboxypropyl)-4-methoxyphenyl)-6,7-dihydro-5h-cyclopenta[b]pyridine-6-carboxylic acid
(5s,6r,7r)-5-(1,3-benzodioxol-5-yl)-2-butyl-7-[2-[(2s)-2-carboxypropyl]-4-methoxyphenyl]-6,7-dihydro-5h-cyclopenta[b]pyridine-6-carboxylic acid
Q27284642

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Endothelin-1 receptorRattus norvegicus (Norway rat)Ki0.00000.00000.00210.0065AID66210
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (3)

Assay IDTitleYearJournalArticle
AID66210Binding affinity towards Endothelin A receptor2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist.
AID66214Selectivity for endothelin A receptor over endothelin receptor B2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist.
AID12753Compound was evaluated for oral bioavailability in rats2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (18)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's4 (22.22)18.2507
2000's13 (72.22)29.6817
2010's1 (5.56)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (5.56%)5.53%
Reviews1 (5.56%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other16 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceDescriptionRelationhip StrengthStudiesTrialsClassesRoles
bosentan anhydrous[no description available]medium21primary alcohol;
pyrimidines;
sulfonamide		antihypertensive agent;
endothelin receptor antagonist
bosentan anhydrous[no description available]medium20primary alcohol;
pyrimidines;
sulfonamide		antihypertensive agent;
endothelin receptor antagonist
tak 044[no description available]medium11
tezosentan[no description available]medium11
atrasentan[no description available]medium11pyrrolidines
lu 135252[no description available]medium11
tbc-11251[no description available]medium11benzodioxoles
bq 123[no description available]medium31cyclic peptide
bq 123[no description available]medium30cyclic peptide
bms 193884[no description available]medium11
endothelin-1[no description available]medium80
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one[no description available]medium10chromones;
morpholines;
organochlorine compound		autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector
sulfobromophthalein[no description available]medium102-benzofurans;
organobromine compound;
organosulfonic acid;
phenols		dye
potassium chloride[no description available]medium10inorganic chloride;
inorganic potassium salt;
potassium salt		fertilizer
y 27632[no description available]medium10aromatic amide
sodium nitrite[no description available]medium10inorganic sodium salt;
nitrite salt		antidote to cyanide poisoning;
antihypertensive agent;
antimicrobial food preservative;
food antioxidant;
poison
thromboxane a2[no description available]medium10epoxy monocarboxylic acid;
thromboxanes A		mouse metabolite
15-hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic acid[no description available]medium10
losartan[no description available]medium10biphenylyltetrazole;
imidazoles		angiotensin receptor antagonist;
anti-arrhythmia drug;
antihypertensive agent;
endothelin receptor antagonist
enrasentan[no description available]medium10aromatic ether;
benzodioxoles;
indanes;
monocarboxylic acid;
monomethoxybenzene;
primary alcohol		antihypertensive agent;
endothelin receptor antagonist
enalaprilat anhydrous[no description available]medium10dicarboxylic acid;
dipeptide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
nitroblue tetrazolium[no description available]medium10organic cation
ConditionIndicatedRelationship StrengthStudiesTrials
Alloxan Diabetes0low20
Anoxemia0low10
Anoxia0low10
Blood Pressure, High0low20
Cardiac Failure0low40
Chronic Disease0low20
Chronic Illness0low20
Chronically Ill0low20
Congestive Heart Failure0low40
Coronary Disease0low10
Coronary Heart Disease0low10
Deficiency, Oxygen0low10
Diabetes Mellitus, Experimental0low20
Experimental Diabetes Mellitus0low20
Heart Decompensation0low40
Heart Disease, Ischemic0low10
Heart Failure0low40
Heart Failure, Congestive0low40
Heart Failure, Left-Sided0low40
Heart Failure, Right-Sided0low40
Hypertension0low20
Hypertension, Pulmonary0low10
Hypoxemia0low10
Hypoxia0low10
Injury, Myocardial Reperfusion0low10
Ischemia, Myocardial0low10
Ischemic Heart Disease0low10
Left-Sided Heart Failure0low40
Muscle Contraction0low10
Muscle Relaxation0low10
Myocardial Failure0low40
Myocardial Ischemia0low10
Myocardial Ischemic Reperfusion Injury0low10
Myocardial Reperfusion Injury0low10
Neointima0low10
Neointima Formation0low10
Oxygen Deficiency0low10
Pulmonary Hypertension0low10
Reperfusion Injury, Myocardial0low10
Right-Sided Heart Failure0low40
Streptozocin Diabetes0low20
Streptozotocin Diabetes0low20

Research Highlights

Long-term Use (1)

ArticleYear
Effects of chronic administration of the novel endothelin antagonist J-104132 on endothelial dysfunction in streptozotocin-induced diabetic rat.
British journal of pharmacology, Volume: 135, Issue: 8		2002
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Pharmacokinetics (1)

ArticleYear
Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist.
Journal of medicinal chemistry, Apr-08, Volume: 47, Issue: 8		2004
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioavailability (2)

ArticleYear
Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist.
Journal of medicinal chemistry, Apr-08, Volume: 47, Issue: 8		2004
Pharmacological properties of J-104132 (L-753,037), a potent, orally active, mixed ETA/ETB endothelin receptor antagonist.
The Journal of pharmacology and experimental therapeutics, Volume: 289, Issue: 3		1999
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Dosage (1)

ArticleYear
Pharmacological properties of J-104132 (L-753,037), a potent, orally active, mixed ETA/ETB endothelin receptor antagonist.
The Journal of pharmacology and experimental therapeutics, Volume: 289, Issue: 3		1999
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]