A192621
A192621 Basic information
- Product Name:
- A192621
- Synonyms:
-
- (2R,3R,4S)-4-(1,3-BENZODIOXOL-5-YL)-1-[2-[(2,6-DIETHYLPHENYL)AMINO]-2-OXOETHYL]-2-(4-PROPOXYPHENYL)PYRROLIDINE-3-CARBOXYLIC ACID
- A192621
- A192621,CID 5310991
- 3-Pyrrolidinecarboxylic acid, 4-(1,3-benzodioxol-5-yl)-1-[2-[(2,6-diethylphenyl)amino]-2-oxoethyl]-2-(4-propoxyphenyl)-, (2R,3R,4S)-
- A192621 >=98 (HPLC)
- CAS:
- 195529-54-5
- MF:
- C33H38N2O6
- MW:
- 558.66
- Mol File:
- 195529-54-5.mol
A192621 Chemical Properties
- 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
A192621 Usage And Synthesis
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. |
IC 50
ETB: 4.5 nM (IC50); ETB: 8.8 nM (Ki); ETA: 4280 nM (IC50); ETA: 5600 nM (Ki)
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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