Page last updated: 2024-11-06

dup 532

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

Description

DuP 532: angiotensin I receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID60770
CHEMBL ID443269
SCHEMBL ID62
SCHEMBL ID23861274
MeSH IDM0188566

Synonyms (30)

Synonym
dup 532
PDSP1_000123
PDSP1_000124
PDSP2_000123
CHEMBL443269 ,
dup-532
5-(1,1,2,2,2-pentafluoroethyl)-2-propyl-3-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylic acid
L002873
cas_124750-95-4
cb91356279
bdbm82428
unii-4bit7v7beo
2-propyl-4-pentafluoroethyl-1-((2'-(1h-tetrazol-5-yl)biphenyl-4-yl)methyl)imidazole-5-carboxylic acid
1h-imidazole-5-carboxylic acid, 4-(pentafluoroethyl)-2-propyl-1-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-
4bit7v7beo ,
124750-95-4
SCHEMBL62
dup532
DTXSID00154476
rqgdxpdtzwgcqi-uhfffaoysa-n
l-694492
1h-imidazole-5-carboxylic acid, 4-(1,1,2,2,2-pentafluoroethyl)-2-propyl-1-((2'-(2h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-
4-(1,1,2,2,2-pentafluoroethyl)-2-propyl-1-((2'-(2h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-1h-imidazole-5-carboxylic acid
l-694,492
2-propyl-4-pentafluoroethyl-1-((2-(1h-tetrazol-5-yl)biphenyl-4-yl)methyl)imidazole-5-carboxylic acid
bdbm50230908
1-((2'-(1h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-4-(perfluoroethyl)-2-propyl-1h-imidazole-5-carboxylic acid
SCHEMBL23861274
1h-imidazole-5-carboxylic acid, 4-(1,1,2,2,2-pentafluoroethyl)-2-propyl-1-[[2'-(2h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-
AKOS040748287

Research Excerpts

Overview

DuP 532 is a novel nonpeptide angiotensin II (AII) receptor antagonist under development for the treatment of hypertension.

ExcerptReferenceRelevance
"DuP 532 is a novel nonpeptide angiotensin II (AII) receptor antagonist under development for the treatment of hypertension. "( DuP 532: a second generation of nonpeptide angiotensin II receptor antagonists.
Carini, DJ; Chiu, AT; Duncia, JV; Leung, KH; McCall, DE; Price, WA; Smith, RD; Timmermans, PB; Wexler, RR; Wong, PC, 1991
)
3.17

Bioavailability

ExcerptReferenceRelevance
" The pharmacokinetics and the effect of the salt form on the bioavailability of DuP 532 were determined in rats and dogs."( The pharmacokinetics and metabolism of DuP 532, a non-peptide angiotensin II receptor antagonist, in rats and dogs.
Burcham, DL; Holm, KA; Huang, SM; Quon, CY; Wong, YN, 1994
)
0.78

Dosage Studied

ExcerptRelevanceReference
" The peptides produced dose-related increases in perfusion pressure, and dose-response curves to all six peptides were parallel."( Analysis of responses to angiotensin peptides in the hindquarters vascular bed of the cat.
Garrison, EA; Kadowitz, PJ; Osei, SY; Santiago, JA, 1995
)
0.29
" Dose-response curves for both peptides were parallel, and the time-to-peak increase in lobar arterial pressure in response to angiotensin IV and angiotensin II was similar whereas the duration of the response to angiotensin IV was significantly shorter."( Analysis of responses to angiotensin IV in the pulmonary vascular bed of the cat.
Cheng, DY; Dent, EL; DeWitt, BJ; Kadowitz, PJ; Nossaman, BD, 1994
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Type-1A angiotensin II receptor Rattus norvegicus (Norway rat)IC50 (µMol)0.00320.00040.15553.8000AID37837; AID37969
Type-1B angiotensin II receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00320.00040.13343.8000AID37837; AID37969
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (9)

Assay IDTitleYearJournalArticle
AID568792Antihypertensive activity in iv dosed renal hypertensive rat model2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID177204Oral effective dose required for lowering blood pressure in renal hypertensive rats (RHR)1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID568790Displacement of radiolabeled angiotensin2 from angiotensin AT1 receptor in rat adrenal cortex membranes2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID37542Potency to antagonize the ability of angiotensin II to contract rabbit aorta1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID39801Evaluation of Angiotensin II antagonistic activity by displacement of [125I]-Sar Ile-AII at the rabbit aorta Angiotensin II receptor, type 11993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Nonpeptide angiotensin II antagonists derived from 1H-pyrazole-5-carboxylates and 4-aryl-1H-imidazole-5-carboxylates.
AID37837Inhibitory activity against Angiotensin II receptor type 1 in rat adrenal membrane1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID37969Tested for inhibitory concentration against AT1 receptor binding affinity in rat liver1993Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16
Nonpeptide angiotensin II receptor antagonists. 2. Design, synthesis, and structure-activity relationships of 2-alkyl-4-(1H-pyrrol-1-yl)-1H-imidazole derivatives: profile of 2-propyl-1-[[2'-(1H-tetrazol-5-yl)-[1,1' -biphenyl]-4-yl]-methyl]-4-[2-(trifluoro
AID177200Intravenous effective dose required for lowering blood pressure in renal hypertensive rats (RHR)1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID568868Antihypertensive activity in po dosed renal hypertensive rat model2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (21)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's19 (90.48)18.2507
2000's1 (4.76)29.6817
2010's1 (4.76)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: 10.93

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 Index10.93 (24.57)
Research Supply Index3.22 (2.92)
Research Growth Index4.15 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.93)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (4.35%)5.53%
Reviews3 (13.04%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other19 (82.61%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]