Lomitapide mesylate

Name: Lomitapide mesylate
Brand: Tocris Bioscience
SKU: 7492

Tocris Bioscience, part of Bio-Techne | Catalog # 7492

COA / SDS

Potent microsomal triglyceride transfer protein (MTP) inhibitor

Key Product Details

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)
Molecular Weight:	789.83

View Full Technical Details for Lomitapide mesylate

Technical Data
Citations

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
InChi Key	QKVKOFVWUHNEBX-UHFFFAOYSA-N
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 for Lomitapide mesylate

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	6.33 mL	31.65 mL	63.30 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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References for Lomitapide mesylate

References are publications that support the biological activity of the product.

Robl A novel series of highly potent benzimidazole-based microsomal triglyceride transfer protein inhibitors. J.Med.Chem. 2001 PMID: 11300866
Sousa Lapatinib, Nilotinib and Lomitapide inhibit haemozoin formation in malaria parasites. Molecules 2020 PMID: 32235391
Wetterau An MTP inhibitor that normalizes atherogenic lipoprotein levels in WHHL rabbits. Science 1998 PMID: 9784135