Lomitapide-d8

A neuropeptide with diverse biological activities

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库存: 现货

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数量
500ug

￥3662.00

2930.00

- +
1mg

￥5862.00

4690.00

- +

已选 0 种 0 瓶

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Background

Lomitapide-d8 is intended for use as an internal standard for the quantification of lomitapide by GC- or LC-MS. Lomitapide is an inhibitor of microsomal triglyceride transfer protein (MTTP; IC50 = 0.5 nM in a triglyceride transfer assay).1 It inhibits apolipoprotein B (ApoB) secretion in HepG2 cells (EC50 = 0.8 nM). Lomitapide inhibits triglyceride secretion in fasted rats (ED50 = 0.19 mg/kg, p.o.) and reduces total plasma cholesterol levels in hamsters (ED50 = 2.4 mg/kg). It also decreases plasma cholesterol and triglyceride levels in the Watanabe-heritable hyperlipidemic (WHHL) rabbit model of homozygous familial hypercholesterolemia when administered at a dose of 10 mg/kg. Formulations containing lomitapide have been used as an adjunct to a low-fat diet and other lipid-lowering treatments in the treatment of homozygous familial hypercholesterolemia.

|1. Wetterau, J.R., Gregg, R.E., Harrity, T.W., et al. An MTP inhibitor that normalizes atherogenic lipoprotein levels in WHHL rabbits. Science 282(5389), 751-754 (1998).