Lomitapide-d4

Lomitapide-d4 (AEGR-733-d4) is deuterium labeled 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

[857296-42-5]

Product Name Alternative

AEGR-733-d4; BMS-201038-d4

UNSPSC

12352005

Target

Isotope-Labeled Compounds; Microsomal Triglyceride Transfer Protein (MTP)

Related Pathways

Metabolic Enzyme/Protease; Others

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Smiles

O=C(C1=C(C2=CC=C(C=C2)C(F)(F)F)C=CC=C1)NC(CC3)CCN3CC([2H])([2H])C([2H])([2H])CC4(C5=CC=CC=C5C6=CC=CC=C64)C(NCC(F)(F)F)=O

Molecular Formula

C39H33D4F6N3O2

Molecular Weight

697.75

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]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.|[3]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.|[4]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.