K-604 dihydrochloride 是酰基辅酶 A：胆固醇酰基转移酶 1 的选择性抑制剂，IC50为 0.45±0.06 μM。

K-604 dihydrochloride is a potent and selective acyl-CoA:cholesterol acyltransferase 1 inhibitor with an IC50 of 0.45±0.06 μM.

a novel ACAT inhibitor, K-604.?The IC(50) values of K-604 for human ACAT-1 and ACAT-2 were 0.45 and 102.85 micromol/L, respectively, indicating that K-604 is 229-fold more selective for ACAT-1.?Kinetic analysis indicated that the inhibition was competitive with respect to oleoyl-coenzyme A with a K(i) value of 0.378 micromol/L.?Exposure of human monocyte-derived macrophages to K-604 inhibited cholesterol esterification with IC(50) of 68.0 nmol/L.?Furthermore, cholesterol efflux from THP-1 macrophages to HDL(3) or apolipoprotein A-I was enhanced by K-604[1].

217094-32-1

C23H32Cl2N6OS3

575.64

DMSO:62.5 mg/mL (108.57 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years