Synonyms: 2-[4-[2-(Benzimidazol-2-ylthio)ethyl]piperazin-1yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide dihydrochloride; 4-[2-(1H-Benzimidazol-2-ylthio)ethyl]-N-[6-methyl-2,4-bis(methylthio)-3-pyridinyl]-1-piperazineacetamide dihydrochloride; K604
Molecular Formula: C23H30N6OS3 · 2HCl
Molecular Weight: 575.64
Linear Structural Formula: C23H30N6OS3 · 2HCl
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: K-604 inhibits against acyl-coenzyme A (acyl-CoA):cholesterol O-acyltransferase-1 (ACAT1, SOAT1) activitiy in a selective (IC50 = 450 nM vs. 102.85 mu M against human ACAT1 and ACAT2, respectively) and acyl-CoA-competitive (Ki = 378 nM against oleoyl-coA) manner. K-604 inhibits cholesterol esterification in human monocyte-derived macrophages (IC50 = 68.0 nM) and enhances cholesterol efflux from THP-1 macrophages in response to HDL3 or apolipoprotein A-I. Oral administration is efficacious against macrophage foam cell formation and atherosclerosis progression among F1B hamsters on a high-fat diet (1-10 mg/kg/day) and apoE-knockout mice (60 mg/kg/day) without affecting plasma cholesterol levels. K-604 is also reported to stimulate autophagy-mediated P301L-Tau degradation in cortical neurons from 3XTg-AD mice (500 nM).