| Description | YM17E is an inhibitor of ACAT with IC50 of 44 nM in rabbit liver microsomes in vitro. |
| In vitro | YM17E在抑制肠道ACAT活性方面具有强效性，其IC50值为34 nM[1]。 |
| In vivo | YM17E以剂量依赖的方式抑制来自[14C]油酰CoA生成[14C]胆固醇油酸酯的过程，适用的酶源为肝脏及肠道微粒体[1]。YM17E（3, 5, 10 mg/kg, 静脉注射）显著以剂量依赖性抑制肝脏ACAT活性。YM17E（口服；静脉注射）显著增加动脉粥样硬化饮食喂养的大鼠的125I-LDL清除率。YM17E（3, 10, 30 mg/kg；口服）剂量依赖性降低总胆固醇、胆固醇酯和非高密度脂蛋白胆固醇水平。YM17E（口服）在剂量依赖性的基础上显著降低肝脏总胆固醇及胆固醇酯水平[2]。 |
| Target activity | ACAT (rabbit liver microsomes):44 nM |
| molecular weight | 652.91 |
| Molecular formula | C40H56N6O2 |
| CAS | 124900-72-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 12 mg/mL (18.38 mM) |
| References | 1. Kashiwa M, et al. Pharmacological properties of YM17E, an acyl-CoA:cholesterol acyltransferase inhibitor, and diarrheal effect in beagle dogs. Jpn J Pharmacol. 1997 Jan;73(1):41-50. 2. Uchida T, et al. Relationship between bioavailability and hypocholesterolemic activity of YM17E, an inhibitor of ACAT, in cholesterol-fed rats. Atherosclerosis. 1998 Mar;137(1):97-106. |