Lomitapide(AEGR-733; BMS-201038)甲磺酸盐是高效MTP蛋白抑制剂，体外IC50值为8nM。
CAS：202914-84-9
分子式：C40H41F6N3O5S
分子量：789.83
纯度：98%
存储：Store at -20°C

Background:

Lomitapide mesylate(AEGR-733; BMS-201038) is an inhibitor of microsomal triglyceride-transfer protein (MTP) wtih in vitro IC50 of 8 nM.IC50 value: 8 nM [1]Target: MTP inhibitorLomitapide is a small-molecule, microsomal triglyceride transfer protein (MTP) inhibitor, for the treatment of both familial and primary hypercholesterolemia. Oral, once-daily lomitapide will be targeted at patients resistant to HMG-CoA reductase inhibitors (statins) either due to abnormalities in liver function or to discontinuation because of muscle pain.

[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]. Lomitapide. Am J Cardiovasc Drugs. 2011 Oct 1;11(5):347-52. [3]. Perry CM. Lomitapide: a review of its use in adults with homozygous familial hypercholesterolemia. Am J Cardiovasc Drugs. 2013 Aug;13(4):285-96.