洛美他派
| 中文名称 | 洛美他派 |
|---|---|
| 中文同义词 | N-(2,2,2-三氟乙基)-9-(4-[4-[4'-(三氟甲基)[1,1'-联苯]-2-甲酰氨基]哌啶-1-基]丁基)-9H-芴-9-甲酰胺;洛美他派;MTP抑制剂(LOMITAPIDE);N-(2,2,2-三氟乙基)-9-(4-[4-[4'-(三氟甲基)[1,1'-联苯]-2-甲酰氨基]哌啶-1-基]丁基)-9H-芴-9-甲酰胺 3级;N-(2,2,2-三氟乙基)-9-(4-[4-[4'-(三氟甲基)[1,1'-联苯]-2-甲酰氨基]哌啶-1-基]丁基)-9H-芴-9-甲酰胺 3级;N-(2,2,2-三氟乙基)-9-(4-[4-[4'-(三氟甲基)[1,1'-联苯]-2-甲酰氨基]哌啶-1-基]丁基)-9H-芴-9-甲酰胺 |
| 英文名称 | Lomitapide |
| 英文同义词 | N-(2,2,2-Trifluoroethyl)-9-(4-[4-[4'-(trifluoromethyl)[1,1'-biphenyl]-2-carboxamido]piperidin-1-yl]butyl)-9H-fluorene-9-carboxamide;N-(2,2,2-trifluoroethyl)-9-[4-[4-[[[4'-(trifluoromethyl)[1,1'-biphenyl]-2-yl]carbonyl]amino]-1-piperidinyl]butyl]-9H-fluorene-9-carboxamide;AEGR 733;BMS 201038;BMS 201038-01;BMS 201238;LoMitapide;N-(2,2,2-trifluoroethyl)-9-(4-(4-(4'-(trifluoroMethyl)biphenyl-2-ylcarboxaMido)piperidin-1-yl)butyl)-9H-fluorene-9-carboxaMide |
| CAS号 | 182431-12-5 |
| 分子式 | C39H37F6N3O2 |
| 分子量 | 693.72 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂，天然产物;细胞生物学试剂;000-中间体;Inhibitors |
| Mol文件 | 182431-12-5.mol |
| 结构式 |  |
洛美他派 性质
| 熔点 | 142°C(lit.) |
|---|---|
| 沸点 | 778.2±60.0 °C(Predicted) |
| 密度 | 1.34±0.1 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | 可溶于DMSO（少许）、甲醇（少许） |
| 酸度系数(pKa) | 12.66±0.20(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| Target | Value |
| MTP |
Lomitapide is an oral microsomal triglyceride transfer protein (MTP) inhibitor indicated for the treatment of patients with HoFH, a rare form of hypercholesterolemia that can lead to premature atherosclerotic disease. Lomitapide undergoes hepatic metabolism via cytochrome P-450 (CYP) isoenzyme 3A4 and interacts with CYP3A4 substrates including atorvastatin and simvastatin.
The use of lomitapide alone or in combination with other lipid-lowering modalities reduces plasma concentrations of low density lipoprotein cholesterol (LDL-C) by a mean of more than 50%. Lomitapide is associated with significant gastrointestinal adverse effects and increases in hepatic fat levels. The bioavailability of the 50-mg lomitapide capsule is 7.1%. The mean half-life of lomitapide is 39.7 hours. Single-dose administration of lomitapide is shown to reduce serum triglycerides by 35% and 47% at 0.3- and 1-mg/kg doses, respectively. Multiple-dose treatment with lomitapide also results in dose dependent decrease in triglycerides (71%–87%), nonesterified fattyacids(33%–40%), and LDL-C(26-29%).
安全信息
| 海关编码 | 2933.39.4100 |
|---|---|
| 毒害物质数据 | 182431-12-5(Hazardous Substances Data) |