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Lomitapide 99%

Lomitapide

源葉(MedMol)
S80485
182431-12-5
C39H37F6N3O2
693.7204
品牌 貨號 產(chǎn)品規(guī)格 價格(RMB) 庫存（上海） 北京 武漢 南京 購買數(shù)量
源葉(MedMol) S80485-5mg 99% ￥510.00元 9 - - -
源葉(MedMol) S80485-10mg 99% ￥850.00元 9 - - -
源葉(MedMol) S80485-50mg 99% ￥2350.00元 6 - - -
源葉(MedMol) S80485-100mg 99% ￥3500.00元 5 - - -
產(chǎn)品介紹 參考文獻 質(zhì)檢證書(COA) 摩爾濃度計算器 相關產(chǎn)品

產(chǎn)品介紹

Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro.
產(chǎn)品描述： Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro.
靶點： IC50: 8 nM (MTP);CETP
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%)
參考文獻：
1. Sulsky R, et al. 5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5067-70. 2. Davis KA. et al. Lomitapide: A novel agent for the treatment of homozygous familial hypercholesterolemia. Am J Health Syst Pharm. 2014 Jun 15;71(12):1001-8. 3. Dhote V, et al. Inhibition of microsomal triglyceride transfer protein improves insulin sensitivity and reduces atherogenic risk in Zucker fatty rats. Clin Exp Pharmacol Physiol. 2011 May;38(5):338-44.
溶解性： soluble  in  DMSO
保存條件： -20℃
配置溶液濃度參考：
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
50 mM 0.029 ml 0.144 ml 0.288 ml
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參考文獻

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