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182431-12-5

中文名稱 N-(2,2,2-三氟乙基)-9-(4-[4-[4'-(三氟甲基)[1,1'-聯(lián)苯]-2-甲酰氨基]哌啶-1-基]丁基)-9H-芴-9-甲酰胺
英文名稱 N-(2,2,2-Trifluoroethyl)-9-(4-[4-[4'-(trifluoromethyl)[1,1'-biphenyl]-2-carboxamido]piperidin-1-yl]butyl)-9H-fluorene-9-carboxamide
CAS 182431-12-5
分子式 C39H37F6N3O2
分子量 693.73
MOL 文件 182431-12-5.mol
更新日期 2024/10/29 10:09:21
182431-12-5 結(jié)構(gòu)式 182431-12-5 結(jié)構(gòu)式

基本信息

中文別名
洛美他派
MTP抑制劑(LOMITAPIDE)
N-(2,2,2-三氟乙基)-9-(4-[4-[4'-(三氟甲基)[1,1'-聯(lián)苯]-2-甲酰氨基]哌啶-1-基]丁基)-9H-芴-9-甲酰胺
英文別名
AEGR 733
BMS 201038
LoMitapide
BMS 201238
BMS 201038-01
AEGR733, BMS201038
AEGR-733(Lomitapide)
CB62485047,loMitapide
Lomitapide (10mM in DMSO)
AEGR-733(Lomitapide)free base

物理化學(xué)性質(zhì)

熔點(diǎn)142°C(lit.)
沸點(diǎn)778.2±60.0 °C(Predicted)
密度1.34±0.1 g/cm3(Predicted)
儲存條件2-8°C
溶解度可溶于DMSO(少許)、甲醇(少許)
酸度系數(shù)(pKa)12.66±0.20(Predicted)
形態(tài)粉末
顏色白色至米色

安全數(shù)據(jù)

海關(guān)編碼2933.39.4100
毒害物質(zhì)數(shù)據(jù)182431-12-5(Hazardous Substances Data)

常見問題列表

生物活性
Lomitapide (AEGR-733, BMS-201038)是一種強(qiáng)效的microsomal triglyceride transfer protein (MTP)抑制劑,用于家族性高膽固醇血癥的治療。
靶點(diǎn)
TargetValue
MTP
體外研究

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.

體內(nèi)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%).

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