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Maraviroc

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产品编号 T6016Cas号 376348-65-1
别名 马拉维若, UK-427857, Selzentry, Celsentri

Maraviroc (Selzentry) 是一种 C-C 趋化因子受体 5 拮抗剂,具有抑制HIV 的活性。

Maraviroc
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Maraviroc

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纯度: 100%
产品编号 T6016 别名 马拉维若, UK-427857, Selzentry, CelsentriCas号 376348-65-1

Maraviroc (Selzentry) 是一种 C-C 趋化因子受体 5 拮抗剂,具有抑制HIV 的活性。

规格价格库存数量
2 mg
¥ 283
现货
5 mg
¥ 429
现货
10 mg
¥ 722
现货
25 mg
¥ 1,470
现货
50 mg
¥ 2,730
现货
100 mg
¥ 3,970
现货
200 mg
¥ 5,790
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500 mg
¥ 8,870
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1 mL x 10 mM (in DMSO)
¥ 515
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产品介绍

生物活性
产品描述
Maraviroc (Selzentry) is a C-C Chemokine Receptor Type 5 (CCR5) antagonist, and for MIP-1α(IC50=3.3 nM), MIP-1β (IC50=7.2 nM) and RANTES(IC50=5.2 nM).Maraviroc inhibits HIV-1 entry via CCR5 coreceptor interaction.
靶点活性
MIP-1α:3.3 nM, RANTES:5.2 nM, MIP-1β:7.2 nM
体外活性
在MIP-1β, MIP-1α和RANTES中,Maraviroc(IC50=7-30 nM)抑制趋化因子诱导的细胞内钙重新分配的下游。
体内活性
在犬类中,口服2 mg/kg Maraviroc,1.5小时后达到峰浓度为256 ng/ml,生物有效性为40%.在大鼠中,Maraviroc半衰期为0.9小时,大约30%给药剂量从肠道吸收.雌性RAG-hu小鼠实验显示,Maraviroc完全保护小鼠免受HIV-1感染.
激酶实验
Inhibition of chemokine binding to CCR5: Binding of 125I-labeled MIP-1α, MIP-1β, and RANTES to CCR5 is measured using intact HEK-293 cells stably expressing the receptor or membrane preparations thereof. Briefly, cells are resuspended in binding buffer (50 mM HEPES containing 1 mM CaCl2, 5 mM MgCl2, and 0.5% bovine serum albumin [BSA] and adjusted to pH 7.4) to a density of 2 × 106 cells/ml. For membrane preparations, phosphate-buffered saline (PBS)-washed cells are resuspended in lysis buffer (20 mM HEPES, 1 mM CaCl2, 1 tablet COMPLETE per 50 mL, pH 7.4) prior to homogenization in a Polytron hand-held homogenizer, ultracentrifugation (40,000× g for 30 min), and resuspension in binding buffer to a protein concentration of 0.25 mg/mL (12.5 μg of membrane protein is used in each well of a 96-well plate). 125I-radiolabeled MIP-1α, MIP-1β, and RANTES are prepared and diluted in binding buffer to a final concentration of 400 pM in the assay. Maraviroc dilutions are added to each well to a final volume of 100 μL, the assay plates incubate for 1 hour, and the contents filter through preblocked and washed Unifilter plates which are counted following overnight drying.
细胞实验
Drug susceptibility assays are performed in 24-well tissue culture plates. Duplicate eight-point dilution series of Maraviroc are prepared in DMSO and medium to yield a final DMSO concentration of 0.1% (vol/vol) in the assay. PHA-stimulated PBMC or PM-1 cells are infected with virus for 1 hour at 37 °C. Cells are subsequently washed once, and 3.6 × 105 PBMC or 2.0 × 105 PM-1 cells are added to each well of assay plates containing diluted Maraviroc. Plates are incubated for 5 days (lab-adapted strains) or 7 days (primary isolates) at 37 °C in a humidified 5% CO2 (vol/vol) atmosphere.(Only for Reference)
别名马拉维若, UK-427857, Selzentry, Celsentri
化学信息
分子量513.67
分子式C29H41F2N5O
CAS No.376348-65-1
SmilesCC(C)c1nnc(C)n1[C@@H]1C[C@@H]2CC[C@H](C1)N2CC[C@H](NC(=O)C1CCC(F)(F)CC1)c1ccccc1
密度1.29 g/cm3 (Predicted)
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: 55 mg/mL (107.07 mM), Sonication is recommended.
Ethanol: 51.4 mg/mL (100.06 mM), Sonication is recommended.
溶液配制表
Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.9468 mL9.7339 mL19.4678 mL97.3388 mL
5 mM0.3894 mL1.9468 mL3.8936 mL19.4678 mL
10 mM0.1947 mL0.9734 mL1.9468 mL9.7339 mL
20 mM0.0973 mL0.4867 mL0.9734 mL4.8669 mL
50 mM0.0389 mL0.1947 mL0.3894 mL1.9468 mL
100 mM0.0195 mL0.0973 mL0.1947 mL0.9734 mL

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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
mg/kg
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

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