| Description | Lopinavir (ABT-378) is a peptidomimetic HIV protease inhibitor that retains activity against HIV protease with the Val 82 mutation. Lopinavir is less affected by binding to serum proteins than the structurally-related drug ritonavir. |
| In vitro | 用Lopinavir（10 mg/kg,p.o.）处理大鼠 ,Cmax为 0.8 μg/mL,该药物生物利用度为25%. |
| In vivo | Lopinavir是Rh123的有效抑制剂,对Caco-2细胞层的IC50为1.7 mM。Lopinavir与突变型 HIV 蛋白酶（V82A, V82T和V82F）结合,Ki分别为4.9、3.7和 3.6 pM。Lopinavir（0.5 nM）可抑制野生型HIV蛋白酶活性（93％）。在有或无50% HS存在时,Lopinavir作用于MT4细胞可抑制HIV蛋白酶活性,EC50 分别为 102和17 nM。在肝微粒中,Lopinavir可转换成初级代谢物M-3和M-4,该过程具有NADPH依赖性。Lopinavir 处理LS 180V 细胞72 h,可降低细胞内Rh123含量,还能诱导P-糖蛋白免疫反应性蛋白和信使RNA水平。 Lopinavir 对C亚型克隆 C6的IC50为9.4 nM。作用于人肝微粒体时,Lopinavir对CYP3A的IC50 为 7.3 mM,对人CYP1A2,2B6,2C9,2C19,2D6也有微弱抑制作用。 |
| Target activity | HIV protease:1.3 pM(Ki) |
| Synonyms | ABT-378, 洛匹那韦 |
| molecular weight | 628.8 |
| Molecular formula | C37H48N4O5 |
| CAS | 192725-17-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: 116 mg/mL (184.5 mM) DMSO: 116 mg/mL (184.5 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) |
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