Lomitapide Mesylate

Names

[ CAS No. ]:
202914-84-9

[ Name ]:
Lomitapide Mesylate

[Synonym ]:
methanesulfonic acid,N-(2,2,2-trifluoroethyl)-9-[4-[4-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]piperidin-1-yl]butyl]fluorene-9-carboxamide
UNII-X4S83CP54E
AEGR-733
Lomitapide mesylate
Juxtapid
Lomitapide (mesylate)

Biological Activity

[Description]:

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.

[Related Catalog]:

Signaling Pathways >> Others >> Others

Research Areas >> Cardiovascular Disease

[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.

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Molecular Formula ]:
C₄₀H₄₁F₆N₃O₅S

[ Molecular Weight ]:
789.82600

[ Exact Mass ]:
789.26700

[ PSA ]:
131.17000

[ LogP ]:
10.31990

[ Storage condition ]:
-20℃

Related Compounds

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