ABT-546

• Description :

  ABT-546 (A-216546), a chemical probe, 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].

• CAS Number :

  [212481-66-8]

• Product Name Alternative :

  A-216546

• UNSPSC :

  12352005

• Hazard Statement :

  H315-H319-H335

• Target :

  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 Formula :

  C30H48N2O6

• Molecular Weight :

  532.71

• Precautions :

  P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P362-P403+P233-P405-P501

• 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

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  ETA