A-192621

• CAT Number: I000182
• CAS Number: 195529-54-5
• Molecular Formula: C33H38N2O6
• Molecular Weight: 558.67
• Purity: ≥95%
• Target: endothelin-B antagonist
• Solubility: Soluble in DMSO, not in water
• Storage: Store at -20°C
• IUPAC Name: (2R,3R,4S)-4-(1,3-benzodioxol-5-yl)-1-[2-(2,6-diethylanilino)-2-oxoethyl]-2-(4-propoxyphenyl)pyrrolidine-3-carboxylic acid
• InChI: InChI=1S/C33H38N2O6/c1-4-16-39-25-13-10-23(11-14-25)32-30(33(37)38)26(24-12-15-27-28(17-24)41-20-40-27)18-35(32)19-29(36)34-31-21(5-2)8-7-9-22(31)6-3/h7-15,17,26,30,32H,4-6,16,18-20H2,1-3H3,(H,34,36)(H,37,38)/t26-,30-,32+/m1/s1
• InChIKey: LQEHCKYYIXQEBM-FUKIBTTHSA-N
• SMILES: CCCOC1=CC=C(C=C1)C2C(C(CN2CC(=O)NC3=C(C=CC=C3CC)CC)C4=CC5=C(C=C4)OCO5)C(=O)O

A-192621 (Cat.No:I000182) is an endothelin-B antagonist. A-192621 markedly enhanced MAP, TPR, and mesenteric, and the renal constrictor effects of ET-1. A-192621 was more effective than IRL-2500 in blocking IRL-1620-induced vasoconstriction, but both augmented constrictor responses to ET-1.

Reference

1:Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: ex vivo and in vivo studies. Wessale JL, Adler AL, Novosad EI, Calzadilla SV, Dayton BD, Marsh KC, Winn M, Jae HS, von Geldern TW, Opgenorth TJ, Wu-Wong JR.Clin Sci (Lond). 2002 Aug;103 Suppl 48:112S-117S. PMID: 12193067 2:Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: in vitro studies. Wu-Wong JR, Dixon DB, Chiou WJ, Sorensen BK, Liu G, Jae HS, Tasker A, von Geldern TW, Winn M, Opgenorth TJ.Clin Sci (Lond). 2002 Aug;103 Suppl 48:107S-111S. PMID: 12193066 3:Use of A-192621 and IRL-2500 to unmask the mesenteric and renal vasodilator role of endothelin ET(B) receptors. Leung SW, Lim SL, Pang CC, Man RY.J Cardiovasc Pharmacol. 2002 Apr;39(4):533-43. PMID: 11904527 4:Use of A-192621 to provide evidence for involvement of endothelin ET(B)-receptors in endothelin-1-mediated cardiomyocyte hypertrophy. Cullen JP, Bell D, Kelso EJ, McDermott BJ.Eur J Pharmacol. 2001 Apr 13;417(3):157-68. PMID: 11334846 5:Effects of A-192621.1, a specific endothelin-B antagonist, on intrarenal hemodynamic responses to endothelin-1. Brodsky S, Abassi Z, Wessale J, Ramadan R, Winaver J, Hoffman A.J Cardiovasc Pharmacol. 2000 Nov;36(5 Suppl 1):S311-3. PMID: 11078406