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| | Lomitapide-d8 Basic information |
| Product Name: | Lomitapide-d8 | | Synonyms: | 9-[1,1,2,2,3,3,4,4-octadeuterio-4-[4-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]piperidin-1-yl]butyl]-N-(2,2,2-trifluoroethyl)fluorene-9-carboxamide | | CAS: | 2459377-96-7 | | MF: | C39H29D8F6N3O2 | | MW: | 701.77 | | EINECS: | | | Product Categories: | | | Mol File: | 2459377-96-7.mol |  |
| | Lomitapide-d8 Chemical Properties |
| Boiling point | 778.174±60.00 °C(Press: 760.00 Torr)(predicted) | | density | 1.341±0.10 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | | solubility | Acetonitrile: soluble | | form | A crystalline solid |
| | Lomitapide-d8 Usage And Synthesis |
| Description | 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. | | Uses | Lomitapide-d8 is deuterium labeled Lomitapide. Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro. | | References | 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). |
| | Lomitapide-d8 Preparation Products And Raw materials |
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