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Lomitapide mesylate is a potent inhibitor of microsomal triglyceride transfer protein (IC50 = 8 nM). Lomitapide inhibits or normalizes lipoprotein production in rodents and in a rabbit model of hypercholesterolemia. Lomitapide is antimalarial; it inhibits hemozoin formation and growth of CQ-sensitive (PfNF54) and multidrug-resistant (PfK1) strains of P. falciparum (IC50 values are 0.56 µM and 0.69 µM respectively). Orally bioavailable.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 789.83. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.2 mM||6.33 mL||31.65 mL||63.3 mL|
|1 mM||1.27 mL||6.33 mL||12.66 mL|
|2 mM||0.63 mL||3.17 mL||6.33 mL|
|10 mM||0.13 mL||0.63 mL||1.27 mL|
References are publications that support the biological activity of the product.
Wetterau et al (1998) An MTP inhibitor that normalizes atherogenic lipoprotein levels in WHHL rabbits. Science 282 751 PMID: 9784135
Robl et al (2001) A novel series of highly potent benzimidazole-based microsomal triglyceride transfer protein inhibitors. J.Med.Chem. 44 856 PMID: 11300866
Sousa et al (2020) Lapatinib, Nilotinib and Lomitapide inhibit haemozoin formation in malaria parasites. Molecules 25 1571 PMID: 32235391
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