Lomitapide

Lomitapide is an inhibitor of microsomal triglyceride transfer protein (MTTP, IC50 = 0.5 nM in a triglyceride transfer assay). 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.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. CAS Number: 182431-12-5. Synonyms: AEGR 773, BMS 201038. Molecular Formula: C39H37F6N3O2. Formula Weight: 693.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 5 mg/ml, Ethanol: 10 mg/ml. lambdamax: 232, 259 nm. SMILES: O=C(NCC(F)(F)F)C1(CCCCN2CCC(NC(C3=CC=CC=C3C4=CC=C(C(F)(F)F)C=C4)=O)CC2)C5=C(C=CC=C5)C6=C1C=CC=C6. InChi Code: InChI=1S/C39H37F6N3O2/c40-38(41,42)25-46-36(50)37(33-13-5-3-10-30(33)31-11-4-6-14-34(31)37)21-7-8-22-48-23-19-28(20-24-48)47-35(49)32-12-2-1-9-29(32)26-15-17-27(18-16-26)39(43,44)45/h1-6,9-18,28H,7-8,19-25H2,(H,46,50)(H,47,49). InChi Key: MBBCVAKAJPKAKM-UHFFFAOYSA-N.