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A-192621 

Cat. No. M29057

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A-192621  Structure

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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 558.66
Formula C33H38N2O6
CAS Number 195529-54-5
Form Solid
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Jerry L Wessale, et al. Clin Sci (Lond). Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: ex vivo and in vivo studies

[2] J Ruth Wu-Wong, et al. Clin Sci (Lond). Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: in vitro studies

[3] Susan Wai Sum Leung, et al. J Cardiovasc Pharmacol. Use of A-192621 and IRL-2500 to unmask the mesenteric and renal vasodilator role of endothelin ET(B) receptors

[4] J P Cullen, et al. Eur J Pharmacol. Use of A-192621 to provide evidence for involvement of endothelin ET(B)-receptors in endothelin-1-mediated cardiomyocyte hypertrophy

[5] S Brodsky, et al. J Cardiovasc Pharmacol. Effects of A-192621.1, a specific endothelin-B antagonist, on intrarenal hemodynamic responses to endothelin-1

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  Catalog
Abmole Inhibitor Catalog




Keywords: A-192621  supplier, Endothelin Receptor, inhibitors, activators

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