Lomitapide mesylate
(Synonyms: 甲磺酸洛美他派; AEGR-733 mesylate; BMS-201038 mesylate) 目录号 : GC36478
An MTTP inhibitor
Cas No.:202914-84-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Lomitapide is an inhibitor of microsomal triglyceride transfer protein (MTTP; IC50 = 0.5 nM in a triglyceride transfer assay).1 It inhibits apolipoprotein B (ApoB) secretion in HepG2 cells (EC50 = 0.8 nM). Lomitapide inhibits triglyceride secretion in fasted rats (ED50 = 0.19 mg/kg, p.o.) and reduces total plasma cholesterol levels in hamsters (ED50 = 2.4 mg/kg). It also decreases plasma cholesterol and triglyceride levels in the Watanabe-heritable hyperlipidemic (WHHL) rabbit model of homozygous familial hypercholesterolemia when administered at a dose of 10 mg/kg. Formulations containing lomitapide have been used as an adjunct to a low-fat diet and other lipid-lowering treatments in the treatment of homozygous familial hypercholesterolemia.
1.Wetterau, J.R., Gregg, R.E., Harrity, T.W., et al.An MTP inhibitor that normalizes atherogenic lipoprotein levels in WHHL rabbitsScience282(5389)751-754(1998)
| Cas No. | 202914-84-9 | SDF | |
| 别名 | 甲磺酸洛美他派; AEGR-733 mesylate; BMS-201038 mesylate | ||
| Canonical SMILES | O=C(C1(CCCCN2CCC(NC(C3=CC=CC=C3C4=CC=C(C(F)(F)F)C=C4)=O)CC2)C5=C(C6=C1C=CC=C6)C=CC=C5)NCC(F)(F)F.O=S(C)(O)=O | ||
| 分子式 | C40H41F6N3O5S | 分子量 | 789.83 |
| 溶解度 | DMSO : ≥ 100 mg/mL (144.15 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2661 mL | 6.3305 mL | 12.661 mL |
| 5 mM | 0.2532 mL | 1.2661 mL | 2.5322 mL |
| 10 mM | 0.1266 mL | 0.633 mL | 1.2661 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Balancing Low-density Lipoprotein Cholesterol Reduction and Hepatotoxicity With Lomitapide mesylate and Mipomersen in Patients With Homozygous Familial Hypercholesterolemia
Rev Cardiovasc Med 2017;18(1):21-28.PMID:28509890DOI:10.3909/ricm0834.
Homozygous familial hypercholesterolemia (HoFH) is an autosomal codominant disorder manifested by high concentrations of total cholesterol and low-density lipoprotein (LDL) cholesterol, and premature cardiovascular disease. Despite conventional lipid-lowering therapy, LDL cholesterol levels remain elevated in patients with HoFH; these patients are considered to be at high risk for cardiovascular events. In 2012-2013, two drugs with novel mechanisms of action were approved by the US Food and Drug Administration for the treatment of HoFH: Lomitapide mesylate and mipomersen. Both of these treatments reduce total cholesterol, LDL cholesterol, non-high-density lipoprotein cholesterol, apolipoprotein B, lipoprotein a, and triglyceride levels. This review describes the clinical tradeoffs in efficacy and hepatotoxicity of these drugs in two cases of HoFH.
Crystal structure of 9-(4-bromo-but-yl)-9H-fluorene-9-carb-oxy-lic acid
Acta Crystallogr Sect E Struct Rep Online 2014 Sep 24;70(Pt 10):o1118-9.PMID:25484705DOI:10.1107/S1600536814019564.
The title compound, C18H17BrO2, is a key inter-mediate in the synthesis of Lomitapide mesylate, a microsomal triglyceride transfer protein inhibitor. Its asymmetric unit contains two independent mol-ecules with slightly different conformations; the mean planes of the 4-bromo-butyl and carboxyl-ate groups in the two mol-ecules form dihedral angles of 24.54 (12) and 17.10 (18)°. In the crystal, carboxyl-ate groups are involved in O-H⋯O hydrogen bonding, which leads to the formation of two crystallographically independent centrosymmetric dimers. Weak inter-molecular C-H⋯O inter-actions further link these dimers into layers parallel to the bc plane.