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ABT-546

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].

Product Specifications

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

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