Lomitapide mesylate |
カタログ番号GC36478 |
Lomitapide mesylate (AEGR-733; BMS-201038) は、8 nM の in vitro IC50 を持つミクロソーム トリグリセリド転送タンパク質 (MTP) の阻害剤です。
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Cas No.: 202914-84-9
Sample solution is provided at 25 µL, 10mM.
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.
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