AEGR-733; BMS-201038 MedChemExpress (MCE)

Product Name	N-(2,2,2-Trifluoroethyl)-9-(4-[4-[4'-(trifluoromethyl)[1,1'-biphenyl]-2-carboxamido]piperidin-1-yl]butyl)-9H-fluorene-9-carboxamide
Synonyms	AEGR 733 AEGR-733 AEGR733 AEGR 733 Lomitapide BMS 201038 BMS201038 Synonyms AEGR 733 AEGR-733 AEGR733 AEGR 733 Lomitapide BMS 201038 BMS201038 BMS 201238 BMS 201038 BMS-201038 BMS 201038-01 AEGR-733(Lomitapide) N-(2,2,2-Trifluoroethyl)-9-(4-[4-[4'-(trifluoromethyl)[1,1'-biphenyl]-2-carboxamido]piperidin-1-yl]butyl)-9H-fluorene-9-carboxamide 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	182431-12-5
EINECS
Chemical Formula	C39H37F6N3O2
Molecular Weight	693.72
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg;25 mg;50 mg;100 mg
Price	Email to quote
Descriptions	Lomitapide Lomitapide MedChemExpress (MCE) HY-14667 182431-12-5 AEGR-733 Descriptions Lomitapide Lomitapide MedChemExpress (MCE) HY-14667 182431-12-5 AEGR-733 BMS-201038 99.60% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. Lomitapide (AEGR-733 BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro. Lomitapide is an oral microsomal triglyceride transfer protein (MTP) inhibitor indicated for the treatment of patients with HoFH, a rare form of hypercholesterolemia that can lead to premature atherosclerotic disease. Lomitapide undergoes hepatic metabolism via cytochrome P-450 (CYP) isoenzyme 3A4 and interacts with CYP3A4 substrates including Atorvastatin (HY-B0589) and Simvastatin (HY-17502)[2]. The use of lomitapide alone or in combination with other lipid-lowering modalities reduces plasma concentrations of low density lipoprotein cholesterol (LDL-C) by a mean of more than 50%. Lomitapide is associated with significant gastrointestinal adverse effects and increases in hepatic fat levels. The bioavailability of the 50-mg lomitapide capsule is 7.1%. The mean half-life of lomitapide is 39.7 hours[2]. Single-dose administration of lomitapide is shown to reduce serum triglycerides by 35% and 47% at 0.3- and 1-mg/kg doses, respectively. Multiple-dose treatment with lomitapide also results in dose dependent decrease in triglycerides (71%–87%), nonesterified fattyacids(33%–40%), and LDL-C(26-29%)[3]. Rats: BMS-201038 is formulated in 0.1% hydroxyl ethyl cellulose and 0.5% Tween 80 in deionized water. Rats in the control group are administered vehicle (2 mL/kg) p.o. Fasted rats are administered 0.3 and 1 mg/kg, p.o., BMS-201038, followed 1 h later by 250 mg/kg, i.v., Triton WR1339. Blood samples are obtained from rats up to 240 min after Triton WR1339 injection to estimate serum triglyceride concentrations. For evaluation of post-prandial lipaemia, fasted rats are administered 0.3 and 1 mg/kg, p.o., BMS-201038, followed 1 h later by a corn oil bolus (6 mL/kg) by oral gavage. Blood samples are again collected up to 1440 min after corn oil administration for the estimation of serum triglyceride concentrations[3]. IC50: 8 nM (MTP)[1] Cellular Effect Cell Line Type Value Description References \| \| \| \| \| \| \| \| \| \| [1]. Sulsky R, et al. 5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP. Bioorg Med Chem Lett. 2004 Oct 18 14(20):5067-70. [Content Brief] [2]. Davis KA. et al. Lomitapide: A novel agent for the treatment of homozygous familial hypercholesterolemia. Am J Health Syst Pharm. 2014 Jun 15 71(12):1001-8. [Content Brief] [3]. Dhote V, et al. Inhibition of microsomal triglyceride transfer protein improves insulin sensitivity and reduces atherogenic risk in Zucker fatty rats. Clin Exp Pharmacol Physiol. 2011 May 38(5):338-44. [Content Brief]
Last Update	2025-04-01 14:45:47

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