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MTTP
/ Lomitapide mesylate

甲磺酸洛美他派 /Lomitapide mesylate {[allProObj[0].p_purity_real_show]}

货号：A615945 同义名： AEGR-733 mesylate;BMS-201038 mesylate Ambeed 开学季，买赠积分，赢豪礼

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.

Lomitapide mesylate 化学结构 CAS号：202914-84-9
Lomitapide mesylate 化学结构
CAS号：202914-84-9
Lomitapide mesylate 3D分子结构
CAS号：202914-84-9
Lomitapide mesylate 化学结构 CAS号：202914-84-9
Lomitapide mesylate 3D分子结构 CAS号：202914-84-9
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Lomitapide mesylate 纯度/质量文件 产品仅供科研

货号：A615945 标准纯度： {[allProObj[0].p_purity_real_show]}
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Lomitapide mesylate 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].

Lomitapide mesylate 参考文献

[1]Perry CM. Lomitapide: a review of its use in adults with homozygous familial hypercholesterolemia. Am J Cardiovasc Drugs. 2013 Aug;13(4):285-96.

[2]Lomitapide. Am J Cardiovasc Drugs. 2011 Oct 1;11(5):347-52.

[3]Jahangir Iqbal,et al. Microsomal Triglyceride Transfer Protein: From Lipid Metabolism to Metabolic Diseases. Adv Exp Med Biol.2020;1276:37-52.

[4]Ekaterina I Biterova,et al. The crystal structure of human microsomal triglyceride transfer protein. Proc Natl Acad Sci U S A. 2019 Aug 27;116(35):17251-17260.

[5]Sulsky R, et al. 5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5067-70.

[6]Caroline M Perry. Lomitapide: a review of its use in adults with homozygous familial hypercholesterolemia. Am J Cardiovasc Drugs. 2013 Aug;13(4):285-96.

[7]Kyle A Davis,et al. Lomitapide: A novel agent for the treatment of homozygous familial hypercholesterolemia. Am J Health Syst Pharm. 2014 Jun 15;71(12):1001-8.

[8]Marina Cuchel,et al. Microsomal transfer protein inhibition in humans. Curr Opin Lipidol. 2013 Jun;24(3):246-50.

Lomitapide mesylate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.27mL

0.25mL

0.13mL

6.33mL

1.27mL

0.63mL

12.66mL

2.53mL

1.27mL

Lomitapide mesylate 技术信息

CAS号202914-84-9
分子式C40H41F6N3O5S
分子量 789.826
别名 AEGR-733 mesylate;BMS-201038 mesylate
运输蓝冰
存储条件

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 105 mg/mL(132.94 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Lomitapide mesylate | AEGR-733 mesylate;BMS-201038 mesylate | MTTP | AmBeed-信号通路专用抑制剂 | Lomitapide mesylate 纯度/质量文件 | Lomitapide mesylate 生物活性 | Lomitapide mesylate 参考文献 | Lomitapide mesylate 实验方案 | Lomitapide mesylate 技术信息

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