Page last updated: 2024-12-08

l 753037

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

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

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Oral bioavailability of J-104132 in rats was approximately 40%."( Pharmacological properties of J-104132 (L-753,037), a potent, orally active, mixed ETA/ETB endothelin receptor antagonist.
Clayton, F; Fukuroda, T; Gabel, R; Hara, K; Hayama, T; Ishikawa, K; Kamei, T; Kanoh, T; Kivlighn, S; Krause, S; Lynch, J; Nishikibe, M; Noguchi, K; Nolan, N; O'Brien, J; Ohta, H; Okada, M; Ozaki, S; Pettibone, D; Saito, M; Siegl, P; William, D; Zingaro, G, 1999
)
0.3
" Here we report an expansion of this work by substituting a variety of electron-withdrawing groups at the ortho position and evaluating their effects on oral bioavailability as well as structure-activity relationships."( 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.
Berens, KL; Blok, N; Bourgoyne, AR; Brock, TA; Bui, H; Decker, ER; Dixon, RA; Holland, GW; Knowles, V; Wang, J; Wu, C; You, TJ, 2004
)
0.32

Dosage Studied

ExcerptRelevanceReference
" In anesthetized dogs, ET-1 was administered directly into the renal artery or brachial artery to generate dose-response (blood flow) curves, and the inhibitory potency of J-104132 (i."( Pharmacological properties of J-104132 (L-753,037), a potent, orally active, mixed ETA/ETB endothelin receptor antagonist.
Clayton, F; Fukuroda, T; Gabel, R; Hara, K; Hayama, T; Ishikawa, K; Kamei, T; Kanoh, T; Kivlighn, S; Krause, S; Lynch, J; Nishikibe, M; Noguchi, K; Nolan, N; O'Brien, J; Ohta, H; Okada, M; Ozaki, S; Pettibone, D; Saito, M; Siegl, P; William, D; Zingaro, G, 1999
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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]

Market Indicators

Research Demand Index: 11.34

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.34 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index4.34 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.34)

All Compounds (24.57)

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]