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ABT-546

CAS No. : 212481-66-8

Biological Activity：ABT-546 (A-216546) is a potent, highly selective and active endothelin ET_A receptor antagonist with a K_i of 0.46 nM for [¹²⁵I]endothelin-1 binding to cloned human endothelin ET_A. ABT-546 is >25,000-fold more selective for the ET_A receptor than for the ET_B receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC₅₀ of 0.59 nM and 3 nM, respectively.

Research Area：Endocrinology|Cardiovascular Disease

Targets：Endothelin Receptor

Related Small Molecules:BQ-788;[Asn18] Endothelin-1, human;Endothelin-3, human, mouse, rabbit, rat TFA;IRL 2500;Sarafotoxin S6c;Sarafotoxin S6a;ANP (1-30), frog;IRL-1620 TFA;Tezosentan;ACT-373898;Ro 46-2005;Ro 46-8443;[Ala2] Endothelin-3, human;ZD-1611;PD-159020;Aminaftone;Aprocitentan-d4;Endothelin 1 (swine, human);Atrial Natriuretic Peptide (ANP) (1-28), rat;Carperitide acetate;[Ala1,3,11,15]-Endothelin (53-63) (TFA);Sparsentan-d5;BQ-123 TFA

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