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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Microsomal Triglyceride Transfer Protein (MTP)-Lomitapide
Lomitapide

Chemical Structure : Lomitapide

CAS No.: 182431-12-5

Lomitapide (AEGR-733, BMS-201038)

货号: PC-24772Not For Human Use, Lab Use Only.

Lomitapide (AEGR-733, BMS-201038) is a highly potent inhibitor of microsomal triglyceride-transfer protein (MTP), inhibits triglyceride transfer of human MTP in vitro with IC50 of 0.5 nM, inhibits secretion of apoB from HepG2 cells with IC50 of 0.8 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Lomitapide (AEGR-733, BMS-201038) is a highly potent inhibitor of microsomal triglyceride-transfer protein (MTP), inhibits triglyceride transfer of human MTP in vitro with IC50 of 0.5 nM, inhibits secretion of apoB from HepG2 cells with IC50 of 0.8 nM.
Lomitapide inhibited the production of lipoprotein particles in rodent models and normalized plasma lipoprotein levels in Watanabe-heritable hyperlipidemic (WHHL) rabbits, which are a model for human homozygous familial hypercholesterolemia.

物理化学性质&存储条件

分子量 693.73
分子式 C39H37F6N3O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(2,2,2-trifluoroethyl)-9-(4-(4-(4'-(trifluoromethyl)-[1,1'-biphenyl]-2-carboxamido)piperidin-1-yl)butyl)-9H-fluorene-9-carboxamide

参考文献

1. Robl JA, et al. J Med Chem. 2001 Mar 15;44(6):851-6.

2. Cuchel M, et al. N Engl J Med. 2007 Jan 11;356(2):148-56.

3. J R Wetterau, et al. Science. 1998 Oct 23;282(5389):751-4.

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