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Evacetrapib

LY2484595,LY 2484595,LY-2484595

Evacetrapib是高活性CETP选择性抑制剂，IC50为5.5 nM，能在不增加醛固酮和血压的情况下提高高密度脂蛋白胆固醇。

目录号
EY1005
EY1005
EY1005
纯度
99.26%
99.26%
99.26%
规格
1 mg
5 mg
10 mg
原价
445
1100
1600
售价
445
1100
1600
库存
现货
现货
现货
订购
订购
订购
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  • 生物活性

    Evacetrapib (LY2484595) is a potent and selective inhibitor of CETP with IC50 of 5.5 nM, elevates HDL cholesterol without increases in aldosterone or blood pressure. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    30 mg/kg 口服处理

  • 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] Cao G, et al. J Lipid Res, 2011, 52(12), 2169-2176.

    分子式
    C31H36F6N6O2    		 分子量
    		 CAS号
    1186486-62-3    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    12.5 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    12.5 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
    NCT02226653 Healthy Volunteers Drug: Evacetrapib Eli Lilly and Company Phase 1 2014-09-01 2015-05-08
    NCT01825889 Cardiovascular Disease Drug: Evacetrapib Eli Lilly and Company Phase 1 2013-04-01 2013-10-30
    NCT01903434 Healthy Volunteers Drug: Evacetrapib Eli Lilly and Company Phase 1 2013-07-01 2014-01-08
    NCT02497391 Healthy Drug: Evacetrapib Eli Lilly and Company Phase 1 2015-07-01 2015-12-15
    NCT02271425 Healthy Volunteers Drug: Evacetrapib Tablet|Drug: Evacetrapib Intravenous Eli Lilly and Company Phase 1 2014-10-01 2014-12-17
    NCT01908582 Healthy Volunteers Drug: Evacetrapib|Drug: Rifampin Eli Lilly and Company Phase 1 2013-07-01 2013-10-30
    NCT02365558 Healthy Drug: Evacetrapib|Drug: Omeprazole Eli Lilly and Company Phase 1 2015-01-01 2015-06-01
    NCT01736254 Healthy Volunteers Drug: Evacetrapib|Drug: Gemfibrozil Eli Lilly and Company Phase 1 2012-12-01 2013-02-14
    NCT02168803 Dyslipidemia Drug: Evacetrapib Eli Lilly and Company Phase 1 2014-05-01 2016-01-25
    NCT01810432 Healthy Volunteers Drug: Evacetrapib|Other: High-fat Meal Eli Lilly and Company Phase 1 2013-03-01 2013-08-23
    NCT02260635 Hypercholesterolemia Drug: Evacetrapib|Drug: Placebo Eli Lilly and Company Phase 3 2014-11-01 2016-08-24
    NCT01836185 Hepatic Insufficiency Drug: Evacetrapib Eli Lilly and Company Phase 1 2013-04-01 2013-10-30
    NCT01687998 Cardiovascular Diseases Drug: Evacetrapib|Drug: Placebo Eli Lilly and Company|The Cleveland Clinic Phase 3 2012-10-01 2016-12-12
    NCT02161731 Healthy Volunteers Drug: Evacetrapib|Drug: Warfarin Eli Lilly and Company Phase 1 2014-06-01 2014-10-09
    NCT01897493 Healthy Volunteers Drug: Evacetrapib|Drug: Digoxin Eli Lilly and Company Phase 1 2013-07-01 2013-09-19
    NCT01825876 Healthy Volunteers Drug: Evacetrapib|Drug: Warfarin Eli Lilly and Company Phase 1 2013-04-01 2013-06-27
    NCT01958489 Healthy Volunteers Drug: Evacetrapib|Drug: Pravastatin Eli Lilly and Company Phase 1 2013-10-01 2014-01-29
    NCT01746732 Healthy Volunteers Drug: Ortho-Cyclen|Drug: Evacetrapib Eli Lilly and Company Phase 1 2012-12-01 2013-06-18
    NCT02156492 Healthy Volunteers Drug: Evacetrapib|Drug: Simvastatin|Drug: Atorvastatin Eli Lilly and Company Phase 1 2014-06-01 2015-01-07
    NCT02260648 Hypercholesterolemia Drug: Evacetrapib|Drug: Ezetimibe|Drug: Atorvastatin|Drug: Placebo Eli Lilly and Company Phase 3 2015-01-01 2016-08-24

    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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