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Evacetrapib

产品编号 T6262Cas号 1186486-62-3
别名 LY2484595

Evacetrapib (LY2484595) 是 CETP 的选择性抑制剂,在人血浆中,抑制人重组 CETP 蛋白 (IC50:5.5 nM) 和 CETP (IC50:36 nM) 活性。

Evacetrapib
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Evacetrapib

纯度: 98.53%
产品编号 T6262 别名 LY2484595Cas号 1186486-62-3

Evacetrapib (LY2484595) 是 CETP 的选择性抑制剂,在人血浆中,抑制人重组 CETP 蛋白 (IC50:5.5 nM) 和 CETP (IC50:36 nM) 活性。

规格价格库存数量
1 mg¥ 213现货
5 mg¥ 483现货
10 mg¥ 818现货
25 mg¥ 1,820现货
50 mg¥ 3,130现货
100 mg¥ 4,480现货
1 mL x 10 mM (in DMSO)¥ 678现货
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纯度:98.53%
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产品介绍

生物活性
产品描述
Evacetrapib (LY2484595) (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.
靶点活性
CETP:5.5 nM
体外活性
Evacetrapib (LY2484595) inhibits human plasma CETP protein with IC50 of 26 nM. Evacetrapib (LY2484595) (< 10 μM) does not induce aldosterone or cortisol synthesis in H295R cells. [1]
体内活性
Evacetrapib (LY2484595) (30 mg/kg, orally) results in 98.4%, 98.6%, and 18.4% inhibition of CETP activity at 4 hours, 8 hours and 24 hours post dose respectively in human ApoAI and CETP double transgenic mice. Evacetrapib (LY2484595) (30 mg/kg) results in 129.7% increase in HDL-C 8 hours after oral administration. The ED50 values of CETP inhibitory activity 8 hours post oral dosing for Evacetrapib (LY2484595) in two dose-response studies are calculated to be 3.5 mg/kg and 4.1 mg/kg respectively. Evacetrapib (LY2484595) (< 200 mg/kg) does not increase blood pressure in Zucker diabetic fatty rats. [1]
激酶实验
Human CETP cDNA is amplified from a human liver cDNA library and the sequence is confirmed to be identical to the published sequence. The cDNA is subcloned into a pcDNA3.1 vector, under the control of CMV promoter. A stable line is established in CV1 cells in which the above-mentioned construct is used to express the recombinant human CETP. The medium contained the secreted recombinant CETP protein and the amount (19 ng/μL) is quantified by an ELISA kit. The medium is then aliquoted in 0.2% BSA and stored at -80°C. The stock CETP protein is diluted 150-fold in CETP buffer (10 mM Tris, 150 mM NaCl, and 2 mM EDTA) before use. The assay is set up in a 96-well plate. Each well received 97.5 μL diluted CETP protein (final concentration 7 nM) and 2.5 μL of compound stock. After a 30 min incubation at 37°C, 5 μL of substrate stock (the same stock used in the human plasma CETP assay), 0.16 μL of VLDL stock (2.5 mg/mL, Intracel) and 145 μL of CETP buffer are added, and the incubation is continued for another 4 h. Signal is read for the human plasma CETP assay[1].
别名LY2484595
化学信息
分子量638.65
分子式C31H36F6N6O2
CAS No.1186486-62-3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 13 mg/mL (20.4 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 11 mg/mL (17.2 mM)
溶液配制表
Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.5658 mL7.8290 mL15.6580 mL78.2901 mL
5 mM0.3132 mL1.5658 mL3.1316 mL15.6580 mL
10 mM0.1566 mL0.7829 mL1.5658 mL7.8290 mL
DMSO
1mg5mg10mg50mg
20 mM0.0783 mL0.3915 mL0.7829 mL3.9145 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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