A-192621

A-192621, a chemical probe, 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].

Product Specifications

CAS Number

[195529-54-5]

UNSPSC

12352005

Target

Apoptosis; Endothelin Receptor

Type

Reference compound

Related Pathways

Apoptosis; GPCR/G Protein

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Endocrinology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/a-192621.html

Purity

99.85

Solubility

DMSO : ≥ 100 mg/mL

Smiles

O=C([C@H]1[C@H](C2=CC=C(OCCC)C=C2)N(CC(NC3=C(CC)C=CC=C3CC)=O)C[C@@H]1C4=CC=C(OCO5)C5=C4)O

Molecular Formula

C33H38N2O6

Molecular Weight

558.66

References & Citations

[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.|[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.|[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.