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ABT-546

Products Details

Product 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].

Web ID

– HY-135283

Shipping

– Room temperature

Applications

– Metabolism-protein/nucleotide metabolism

Molecular Formula

– C30H48N2O6

References

– [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.

CAS Number

– 212481-66-8

Molecular Weight

– 532.71

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

Clinical Information

– No Development Reported

Research Area

– Endocrinology; Cardiovascular Disease

Solubility

– 10 mM in DMSO

Target

– Endothelin Receptor

Isoform

– ETA

Pathway

– GPCR/G Protein

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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