2-(4-(2-(1H-benzo[d]imidazol-2-ylthio)ethyl)piperazin-1-yl)-N-(6-methyl-2,4-bis(methylthio)pyridin-3-yl)acetamide

A potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor with an IC50 of 0.45±0.06 µM

OTAVAchemicals Catalogue Number: 7070707145

CAS Registry Number: 561023-90-3

Purity: 97% (HPLC)

Ref.: Discovery of Clinical Candidate 2-(4-(2-((1H-Benzo[d]imidazol-2-yl)thio)ethyl)piperazin-1-yl)-N-(6-methyl-2,4-bis(methylthio)pyridin-3-yl)acetamide Hydrochloride [K-604], an Aqueous-Soluble Acyl-CoA:Cholesterol O-Acyltransferase-1 Inhibitor.Kimiyuki Shibuya, Katsumi Kawamine, Chiyoka Ozaki, Tadaaki Ohgiya, Toshiyuki Edano, Yasunobu Yoshinaka, and Yoshihiko Tsunenari.J. Med. Chem. 2018, 61, 23, 10635-10650

Abstract: 2-(4-(2-((1H-Benzo[d]imidazol-2-yl)thio)- ethyl)piperazin-1-yl)-N-(6-methyl-2,4-bis(methylthio)- pyridin-3-yl)acetamide hydrochloride (K-604, ) has been identified as an aqueous-soluble potent inhibitor of human acyl-coenzyme A:cholesterol O-acyltransferase (ACAT, also known as SOAT)-1 that exhibits 229-fold selectivity for human ACAT-1 over human ACAT-2.

 https://doi.org/10.1021/acs.jmedchem.8b01256

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