Lomitapide mesylate

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Description: Potent microsomal triglyceride transfer protein (MTP) inhibitor
Chemical Name: N-(2,2,2-Trifluoroethyl)-9-[4-[4-[[[4'-(trifluoromethyl)[1,1'-biphenyl]-2-yl]carbonyl]amino]-1-piperidinyl]butyl]-9H-fluorene-9-carboxamide methanesulfonate
Purity: ≥98% (HPLC)

Biological Activity for Lomitapide mesylate

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.

Technical Data for Lomitapide mesylate

M. Wt 789.83
Formula C39H37F6N3O2.CH3SO3H
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2059395-52-5
PubChem ID 11274333
Smiles O=C(C1=C(C2=CC=C(C(F)(F)F)C=C2)C=CC=C1)NC3CCN(CC3)CCCCC4(C5=C(C6=C4C=CC=C6)C=CC=C5)C(NCC(F)(F)F)=O.CS(O)(=O)=O

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.

Solubility Data for Lomitapide mesylate

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 15.8 20
ethanol 7.9 10

Preparing Stock Solutions for Lomitapide mesylate

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for Lomitapide mesylate

References for Lomitapide mesylate

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

If you know of a relevant reference for Lomitapide mesylate, please let us know.

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Citations for Lomitapide mesylate

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