| Description | Mevastatin (ML236B) is an HMG-CoA reductase inhibitor that was initially isolated from the mold Pythium ultimum. Mevastatin was the first statin to enter clinical trials. |
| In vitro | Mevastatin通过竞争性抑制HMG-CoA还原酶抑制肝脏产生胆固醇.在14天高剂量治疗后,基线绝对脑血流量高出30％.口服给药5 mg/kg和20 mg/kg Mevastatin,3小时后会降低血清胆固醇水平.20 mg/kg Mevastatin能够降低大约30%的血清胆固醇水平. |
| In vivo | Mevastatin的二环部分与辅酶A的活性位点结合。Mevastatin增加eNOS mRNA 和蛋白质水平,减少梗死面积,并以剂量和时间依赖方式改善神经功能缺损。在0.01 pg/mL (26 nM)浓度下,与对照组相比,Mevastatin能够降低50%的胆固醇合成。 |
| Target activity | HMG-CoA reductase:1 nM(ki) |
| Synonyms | Compactin, ML236B, 美伐他汀 |
| molecular weight | 390.51 |
| Molecular formula | C23H34O5 |
| CAS | 73573-88-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 72 mg/mL (184.4 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Endo A, et al. J Antibiot (Tokyo), 1976, 29(12), 1346-1348. 2. Amin-Hanjani S, et al. Stroke, 2001, 32(4), 980-986. |