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 μ 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).
- UPC:
- 51322400
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- SML1837-25MG
- CAS:
- 217094-32-1
