Lomitapide

Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro.

Product Specifications

CAS Number

[182431-12-5]

Product Name Alternative

AEGR-733; BMS-201038

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Microsomal Triglyceride Transfer Protein (MTP)

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/Lomitapide.html

Concentration

10mM

Purity

99.63

Solubility

DMSO : ≥ 100 mg/mL

Smiles

O=C(C1(CCCCN2CCC(NC(C3=CC=CC=C3C4=CC=C(C(F)(F)F)C=C4)=O)CC2)C5=C(C6=C1C=CC=C6)C=CC=C5)NCC(F)(F)F

Molecular Formula

C39H37F6N3O2

Molecular Weight

693.72

Precautions

H302, H315, H319, H335

References & Citations

[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.