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Lomitapide

洛美他派

Lomitapide(AEGR-733, BMS-201038)是一种高效MTP蛋白抑制剂，体外IC50值为8nM。

目录号
EY1382
EY1382
EY1382
EY1382
EY1382
纯度
99.55%
99.55%
99.55%
99.55%
99.55%
规格
1 mg
5 mg
10 mg
50 mg
100 mg
原价
275
750
1060
2600
4100
售价
275
750
1060
2600
4100
库存
现货
现货
现货
现货
现货
订购
订购
订购
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  • 生物活性

    Lomitapide is a potent microsomal triglyceride transfer protein (MTP) inhibitor, used in the treatment of familial hypercholesterolemia.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] M Cuchel,et al.Lomitapide is an inhibitor of microsomal triglyceride transfer protein (MTP). Lomitapide has been shown to be highly effective in reducing LDL-cholesterol and triglycerides, and has been aproved for treatment of homozygous familial hypercholesterolemia. Lancet. Author manuscript; available in PMC 2015 Sep 29. Published in final edited form as: Lancet. 2013 Jan 5; 381(9860): 40–46. Published online 2012 Nov 2. doi: 10.1016/S0140-6736(12)61731-0.

    分子式
    C39H37F6N3O2    		 分子量
    693.72    		 CAS号
    182431-12-5    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    100 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02080455 Effect of Atorvastatin on the Pharmacokinetics of Lomitapide Drug: lomitapide|Drug: Atorvastatin Aegerion Pharmaceuticals, Inc. Phase 1 2014-02-01 2015-03-23
    NCT02173158 Familial Hypercholesterolemia - Homozygous Drug: lomitapide Aegerion Pharmaceuticals, Inc. Phase 3 2014-04-01 2015-06-17
    NCT02044419 Healthy Drug: lomitapide Aegerion Pharmaceuticals, Inc. Phase 1 2013-10-01 2014-01-22
    NCT02135705 Homozygous Familial Hypercholesterolemia Drug: Lomitapide Aegerion Pharmaceuticals, Inc. 2014-03-01 2014-05-08
    NCT00943306 Familial Hypercholesterolemia Drug: lomitapide Aegerion Pharmaceuticals, Inc. Phase 3 2009-09-01 2015-03-26
    NCT02080468 Healthy Drug: lomitapide|Drug: EE/norgestimate Aegerion Pharmaceuticals, Inc. Phase 1 2014-02-01 2015-03-23
    NCT01915771 Intra-subject Variability of Pharmacokinetics Drug: lomitapide Aegerion Pharmaceuticals, Inc. Phase 1 2013-08-01 2014-06-23
    NCT02765841 Homozygous Familial Hypercholesterolemia Drug: Lomitapide Aegerion Pharmaceuticals, Inc. Phase 3 2016-05-01 2016-09-01
    NCT02399839 Pregnancy Drug: lomitapide Aegerion Pharmaceuticals, Inc. 2014-10-01 2016-01-13
    NCT02399852 Homozygous Familial Hypercholesterolemia Drug: Lomitapide Aegerion Pharmaceuticals, Inc. 2015-04-01 2015-03-25
    NCT01760187 Healthy Volunteer Drug: lomitapide Aegerion Pharmaceuticals, Inc.|Richmond Pharmacology Limited Phase 1 2012-11-01 2014-01-21
    NCT01556906 Homozygous Familial Hypercholesterolemia Drug: Lomitapide Aegerion Pharmaceuticals, Inc.|University of Pennsylvania|Doris Duke Charitable Foundation Phase 2 2003-06-01 2013-04-04
    NCT00730236 Homozygous Familial Hypercholesterolemia Drug: AEGR-733 Aegerion Pharmaceuticals, Inc.|FDA Office of Orphan Products Development Phase 3 2007-12-01 2014-01-15
    NCT00690443 Hypercholesterolemia Drug: Atorvastatin|Drug: AEGR-733 Aegerion Pharmaceuticals, Inc. Phase 2 2008-05-01 2013-04-04
    NCT00405067 Hypercholesterolemia Drug: BMS-201038 (AEGR-733)|Drug: Ezetimibe Aegerion Pharmaceuticals, Inc. Phase 2 2006-05-01 2014-01-15
    NCT00359281 Healthy Drug: atorvastatin|Drug: simvastatin|Drug: ezetimibe|Drug: fenofibrate|Drug: dextromethorphan|Drug: Extended Release Niacin Aegerion Pharmaceuticals, Inc. Phase 2 2006-03-01 2014-01-15
    NCT00559962 Hyperlipidemia Drug: AEGR-733|Drug: placebo|Drug: AEGR-733|Drug: AEGR-733|Drug: AEGR-733|Drug: AEGR-733 and atorvastatin|Drug: AEGR-733 and fenofibrate|Drug: AEGR-733 and ezetimibe Aegerion Pharmaceuticals, Inc. Phase 2 2007-10-01 2014-01-15
    NCT00474240 Hypercholesterolemia Drug: Atorvastatin 20 mg|Drug: AEGR-733 5 mg|Drug: AEGR-733 10 mg|Drug: Placebo|Drug: AEGR-733 5 mg + atorvastatin 20 mg|Drug: AEGR-733 10 mg + atorvastatin 20 mg Aegerion Pharmaceuticals, Inc. Phase 2 2007-04-01 2014-01-15

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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