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CAS No.: 202914-84-9

甲磺酸洛美他派 Catalog No. CSN18087

Synonyms: AEGR-733 mesylate;BMS-201038 mesylate;AEGR-733

Lomitapide Mesylate is a MTTP inhibitor with IC50 of 8 nM, used as a complement to a low-fat diet and other lipid-lowering treatments in patients with homozygous familial hypercholesterolemia.

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生物活性

描述Microsomal triglyceride transfer protein (MTP) is a multifunctional protein, and its deregulation during pathophysiological conditions gives rise to different metabolic conditions^[3]. MTP plays an essential role in lipid metabolism, especially in the biogenesis of very low-density lipoproteins and chylomicrons via the transfer of neutral lipids and the assembly of apoB-containing lipoproteins^[4]. Lomitapide is a small-molecule, 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^[5]. Lomitapide is an orally administered inhibitor of the microsomal triglyceride transfer protein, inhibits the synthesis of chylomicrons and very low-density lipoprotein, thereby reducing plasma levels of low-density lipoprotein cholesterol (LDL-C)^[6]. Lomitapide undergoes hepatic metabolism via cytochrome P-450 (CYP) isoenzyme 3A4 and interacts with CYP3A4 substrates including atorvastatin and simvastatin; dose adjustment is recommended when lomitapide is used concurrently with these agents^[7]. In the presence of an up-titration regiment and low-fat diet, lomitapide is generally well tolerated and liver fat accumulation stabilizes after the initial increase. Elevation of alanine aminotranferase levels greater than 3 times the upper limit of normal can be managed successfully with temporary dose reduction^[8].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.2661 mL
- 6.3305 mL
- 12.6610 mL
- 5 mM
- 0.2532 mL
- 1.2661 mL
- 2.5322 mL
- 10 mM
- 0.1266 mL
- 0.6331 mL
- 1.2661 mL

技术信息

CAS号

202914-84-9

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C40H41F6N3O5S

运输

蓝冰

分子量

789.83

别名

AEGR-733 mesylate;BMS-201038 mesylate;AEGR-733;BMS-201038;Lojuxta;甲磺酸洛美他派

溶解度

DMSO	420.0 mg/mL (531.8 mM)
Water	insoluble

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