An MTTP inhibitor (IC50 = 0.5 nM in a triglyceride transfer assay); inhibits ApoB secretion in HepG2 cells (EC50 = 0.8 nM); inhibits triglyceride secretion in fasted rats (ED50 = 0.19 mg/kg

Lomitapide – 5 mg

Brand:
Cayman
CAS:
182431-12-5
Storage:
-20
UN-No:
Non-Hazardous - /

Lomitapide is an inhibitor of microsomal triglyceride transfer protein (MTTP; IC50 = 0.5 nM in a triglyceride transfer assay).{6754} 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.  

 

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SKU: 10009610 - 5 mg Category:

Description

An MTTP inhibitor (IC50 = 0.5 nM in a triglyceride transfer assay); inhibits ApoB secretion in HepG2 cells (EC50 = 0.8 nM); inhibits triglyceride secretion in fasted rats (ED50 = 0.19 mg/kg, p.o.); reduces total plasma cholesterol levels in hamsters (ED50 = 2.4 mg/kg); decreases plasma cholesterol and triglyceride levels in the WHHL rabbit model of homozygous familial hypercholesterolemia at 10 mg/kg

Formal name: N-(2,2,2-trifluoroethyl)-9-[4-[4-[[[4′-(trifluoromethyl)[1,1′-biphenyl]-2-yl]carbonyl]amino]-1-piperidinyl]butyl]-9H-fluorene-9-carboxamide

Synonyms:  AEGR 773|BMS 201038

Molecular weight: 693.7

CAS: 182431-12-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cardiovascular System|Lipids & Lipoproteins||Research Area|Endocrinology & Metabolism|Inborn Errors of Metabolism||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Dyslipidemias||Research Area|Lipid Biochemistry|Glycerolipids||Research Area|Lipid Biochemistry|Sterol Lipids

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