| Description | K-604 dihydrochloride is a potent and selective acyl-CoA:cholesterol acyltransferase 1 inhibitor with an IC50 of 0.45±0.06 μM. |
| In vitro | 一种新颖的ACAT抑制剂K-604对人类ACAT-1和ACAT-2的IC(50)值分别为0.45µM和102.85µM。示K-604对ACAT-1的选择性是对ACAT-2的229倍。动力学分析表明，与油酰辅酶A相比，抑制作用为竞争性，其K(i)值为0.378µM。人类单核细胞衍生的巨噬细胞暴露于K-604时，胆固醇酯化作用被抑制，IC(50)为68.0nM。进一步，K-604增强了THP-1巨噬细胞向HDL(3)或载脂蛋白A-I的胆固醇逆向运输[1]。 |
| Target activity | ACAT1:0.45 μM, ACAT2:102.85 μM |
| molecular weight | 575.64 |
| Molecular formula | C23H32Cl2N6OS3 |
| CAS | 217094-32-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 62.5 mg/mL (108.57 mM), Sonication is recommended. |
| References | 1. Ikenoya M, et al. A selective ACAT-1 inhibitor, K-604, suppresses fatty streak lesions in fat-fed hamsters without affecting plasma cholesterol levels. Atherosclerosis. 2007 Apr;191(2):290-7. 2. Shibuya Y, et al. Acyl-coenzyme A:cholesterol acyltransferase 1 blockage enhances autophagy in the neurons of triple transgenic Alzheimer's disease mouse and reduces human P301L-tau content at the presymptomatic stage. Neurobiol Aging. 2015 Jul;36(7):2248-2259. |