中文名 | 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 | N-(2,2,2-Trifluoroethyl)-9-(4-[4-[4'-(trifluoromethyl)[1,1'-biphenyl]-2-carboxamido]piperidin-1-yl]butyl)-9H-fluorene-9-carboxamide |
别名 | 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 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 |
英文别名 | AEGR 733 AEGR-733 AEGR733 AEGR 733 Lomitapide BMS 201038 BMS201038 BMS 201238 BMS 201038 BMS-201038 BMS 201038-01 AEGR-733(Lomitapide) 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 |
CAS | 182431-12-5 |
化学式 | C39H37F6N3O2 |
分子量 | 693.72 |
密度 | 1.34±0.1 g/cm3(Predicted) |
熔点 | 142°C(lit.) |
沸点 | 778.2±60.0 °C(Predicted) |
溶解度 | DMSO (微溶) 、甲醇 (微溶) |
酸度系数 | 12.66±0.20(Predicted) |
存储条件 | 2-8°C |
外观 | 粉末 |
颜色 | white to beige |
体外研究 | 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. |
体内研究 | 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%). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.442 ml | 7.208 ml | 14.415 ml |
5 mM | 0.288 ml | 1.442 ml | 2.883 ml |
10 mM | 0.144 ml | 0.721 ml | 1.442 ml |
5 mM | 0.029 ml | 0.144 ml | 0.288 ml |
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