Lomitapide mesylate

Cat. No. 7492 提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent microsomal triglyceride transfer protein (MTP) inhibitor

化学名： 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

纯度： ≥98% (HPLC)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 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.

技术数据 for Lomitapide mesylate

分子量	789.83
公式	C₃₉H₃₇F₆N₃O₂.CH₃SO₃H
储存	Store at -20°C
纯度	≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Lomitapide mesylate

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	DMSO	15.8	20
	ethanol	7.9	10

制备储备液 for Lomitapide mesylate

以下数据基于产品分子量 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.

浓度/溶剂体积/质量	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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产品说明书 for Lomitapide mesylate

分析证书/产品说明书

化学品安全技术说明书

参考文献 for Lomitapide mesylate

参考文献是支持产品生物活性的出版物。

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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