| Identification | Back Directory | [Name]
A192621 | [CAS]
195529-54-5 | [Synonyms]
A192621
A192621,CID 5310991
A192621 >=98 (HPLC)
(2R,3R,4S)-4-(1,3-BENZODIOXOL-5-YL)-1-[2-[(2,6-DIETHYLPHENYL)AMINO]-2-OXOETHYL]-2-(4-PROPOXYPHENYL)PYRROLIDINE-3-CARBOXYLIC ACID
3-Pyrrolidinecarboxylic acid, 4-(1,3-benzodioxol-5-yl)-1-[2-[(2,6-diethylphenyl)amino]-2-oxoethyl]-2-(4-propoxyphenyl)-, (2R,3R,4S)- | [Molecular Formula]
C33H38N2O6 | [MDL Number]
MFCD05662209 | [MOL File]
195529-54-5.mol | [Molecular Weight]
558.66 |
| Chemical Properties | Back Directory | [Boiling point ]
738.3±60.0 °C(Predicted) | [density ]
1.233±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
powder | [pka]
3.52±0.60(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level[1][2][3]. | [Biological Activity]
A192621 is a selective; orally available ETB endothelin receptor antagonist. A192621 has been shown to cause an increase in arterial blood pressure and to promote apoptosis in human pulmonary arterial smooth muscle cells. | [in vivo]
A-192621 (30-100 mg/kg; oral administration; daily; for 3 days; male Sprague-Dawley rats) treatment inhibits both dilatory and pressor responses induced by S6c mediated by ETB with an ED50 value of 30 mg/kg, and failed to inhibit the ET-1-induced pressor response mediated by ETA. A-192621 alone causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level in the conscious normotensive rat[3]. | Animal Model: | Male Sprague-Dawley rats (250-350 g)[3] | | Dosage: | 30 mg/kg 100 mg/kg | | Administration: | Oral administration; daily; for 3 days | | Result: | Inhibited both dilatory and pressor responses induced by S6c mediated by ETB with an ED50value of 30 mg/kg.
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| [IC 50]
ETB: 4.5 nM (IC50); ETB: 8.8 nM (Ki); ETA: 4280 nM (IC50); ETA: 5600 nM (Ki) | [storage]
Store at -20°C | [References]
[1] Wu-Wong JR, et al. Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: in vitro studies. Clin Sci (Lond). 2002 Aug;103 Suppl 48:107S-111S. DOI:10.1042/CS103S107S
[2] Sakai S, et al. Antagonists to endothelin receptor type B promote apoptosis in human pulmonary arterial smooth muscle cells. Life Sci. 2016 Aug 15;159:116-120. DOI:10.1016/j.lfs.2016.03.044
[3] Wessale JL, et al. Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: ex vivo and in vivo studies. Clin Sci (Lond). 2002 Aug;103 Suppl 48:112S-117S. DOI:10.1042/CS103S112S |
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MedChemExpress
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