ABT-546

• UNSPSC Description:

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

• Target Antigen:

  Endothelin Receptor

• Type:

  Reference compound

• Related Pathways:

  GPCR/G Protein

• Applications:

  Metabolism-protein/nucleotide metabolism

• Field of Research:

  Endocrinology; Cardiovascular Disease

• Assay Protocol:

  https://www.medchemexpress.com/abt-546.html

• Solubility:

  10 mM in DMSO

• Smiles:

  O=C([C@H]1[C@H](CC(C)(C)CCC)N(CC(N(CCCC)CCCC)=O)C[C@@H]1C2=CC(OC)=C(OCO3)C3=C2)O

• Molecular Weight:

  532.71

• References & Citations:

  [1]u-Wong JR, et al. Pharmacology of A-216546: a highly selective antagonist for endothelin ET(A) receptor. Eur J Pharmacol. 1999 Feb 5;366(2-3):189-201.

• Shipping Conditions:

  Room temperature

• Clinical Information:

  No Development Reported

• CAS Number:

  212481-66-8