产品说明书
Lomitapide mesylate
 |
同义名 : | AEGR-733 mesylate;BMS-201038 mesylate |
| CAS号 : | 202914-84-9 | |
| 货号 : | A615945 | |
| 分子式 : | C40H41F6N3O5S | |
| 纯度 : | 98% | |
| 分子量 : | 789.83 | |
| MDL号 : | MFCD19443682 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 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 |
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| 动物实验配方： |
| 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]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.27mL 0.25mL 0.13mL |
6.33mL 1.27mL 0.63mL |
12.66mL 2.53mL 1.27mL |
| 参考文献 |
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[2]Lomitapide. Am J Cardiovasc Drugs. 2011 Oct 1;11(5):347-52. |