貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S80485-5mg	99.4%	￥510.00 S80485-5mg ￥510.00 現(xiàn)貨	9 9	-	-	-
S80485-10mg	99.4%	￥850.00 S80485-10mg ￥850.00 現(xiàn)貨	9 9	-	-	-
S80485-50mg	99.4%	￥2350.00 S80485-50mg ￥2350.00 現(xiàn)貨	6 6	-	-	-
S80485-100mg	99.4%	￥3500.00 S80485-100mg ￥3500.00 現(xiàn)貨	5 5	-	-	-

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(diǎn)：

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(xiàn)：

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

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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Lomitapide