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Lomitapide

Catalog No. T6267 CAS 182431-12-5

Synonyms: AEGR-733, BMS-201038

Lomitapide (AEGR-733) is a small molecule inhibitor of microsomal triglyceride transfer protein (MTP), an enzyme located in the lumen of the endoplasmic reticulum responsible for absorbing dietary lipids and transferring triglycerides onto apolipoprotein B (apo-B) in the assembly of very-low-density lipoprotein.

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Lomitapide, CAS 182431-12-5

Pack Size	Availability	Price/USD
2 mg	In stock	$ 59.00
5 mg	In stock	$ 96.00
10 mg	In stock	$ 148.00
25 mg	In stock	$ 243.00
50 mg	In stock	$ 349.00
100 mg	In stock	$ 525.00
200 mg	In stock	$ 754.00
500 mg	In stock	$ 1,160.00
1 mL * 10 mM (in DMSO)	In stock	$ 164.00

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Purity: 99.77%

Purity: 99.23%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Lomitapide (AEGR-733) is a small molecule inhibitor of microsomal triglyceride transfer protein (MTP), an enzyme located in the lumen of the endoplasmic reticulum responsible for absorbing dietary lipids and transferring triglycerides onto apolipoprotein B (apo-B) in the assembly of very-low-density lipoprotein.
Targets&IC50	MTP: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 through cytochrome P-450 (CYP) isoenzyme 3A4 and interacts with CYP3A4 substrates including atorvastatin and simvastatin[2].
In vivo	Lomitapide, either as monotherapy or in combination with other lipid-lowering agents, notably reduces low-density lipoprotein cholesterol (LDL-C) levels by over 50%. However, its use is accompanied by significant gastrointestinal side effects and increased hepatic fat. The 50-mg capsule of lomitapide has a bioavailability of 7.1%, and its mean half-life is approximately 39.7 hours[2]. Administration of a single dose of lomitapide can decrease serum triglycerides by 35% and 47% at dosages of 0.3 and 1 mg/kg, respectively. Moreover, multiple-dose regimens have shown a dose-dependent reduction in triglycerides (71%-87%), nonesterified fatty acids (33%-40%), and LDL-C (26-29%)[3].

Synonyms	AEGR-733, BMS-201038
Molecular Weight	693.72
Formula	C39H37F6N3O2
CAS No.	182431-12-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 93 mg/mL (134.3 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 93 mg/mL (134.3 mM)

References and Literature

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. 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. 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.

Related compound libraries

This product is contained In the following compound libraries：

EMA Approved Drug Library Drug Repurposing Compound Library Inhibitor Library Clinical Compound Library Bioactive Compounds Library Max Anti-Metabolism Disease Compound Library Orally Active Compound Library Fluorochemical Library NO PAINS Compound Library Anti-COVID-19 Compound Library

Related Products

Related compounds with same targets

TAP311 Torcetrapib Evacetrapib Dalcetrapib CP-532623 Implitapide Lomitapide Mesylate Granotapide

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Keywords

Lomitapide 182431-12-5 Metabolism CETP AEGR 733 BMS 201038 Inhibitor AEGR733 BMS201038 AEGR-733 inhibit BMS-201038 inhibitor

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