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Maraviroc

Maraviroc

产品编号 T6016   CAS 376348-65-1
别名: Celsentri, Selzentry, 马拉维若, UK-427857

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

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Maraviroc, CAS 376348-65-1
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产品目录号及名称: Maraviroc (T6016)
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纯度: 100%
纯度: 99.55%
纯度: 99.21%
纯度: 98.53%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Maraviroc 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.
体内活性 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。
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 Celsentri, Selzentry, 马拉维若, UK-427857
分子量 513.67
分子式 C29H41F2N5O
CAS No. 376348-65-1

存储

 | Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

DMSO: 38.5 mg/mL (75 mM)

Ethanol: 51.4 mg/mL (100 mM)

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Dorr P, et al. Antimicrob Agents Chemother. 2005, 49(11), 4721-4732. 2. Neff CP, et al. PLoS One. 2011, 6(6), e20209. 3. Tan S, Li J Q, Cheng H, et al. The anti-parasitic drug suramin potently inhibits formation of seminal amyloid fibrils and their interaction with HIV-1[J]. Journal of Biological Chemistry. 2019: jbc. RA118. 006797. 4. Yang J Y, Zhang J, Lu R, et al. T cell–derived exosomes induced macrophage inflammatory protein‐1α/β drive the trafficking of CD8+ T cells in oral lichen planus[J]. Journal of cellular and molecular medicine. 2020

文献引用

1. Yang J Y, Zhang J, Lu R, et al. T cell–derived exosomes induced macrophage inflammatory protein‐1α/β drive the trafficking of CD8+ T cells in oral lichen planus. Journal of Cellular and Molecular Medicine. 2020 2. Tan S, Li J Q, Cheng H, et al. The anti-parasitic drug suramin potently inhibits formation of seminal amyloid fibrils and their interaction with HIV-1. Journal of Biological Chemistry. 2019: jbc. RA118. 006797 3. Wu Q, Cui L, Ma W, et al.A novel small-molecular CCR5 antagonist promotes neural repair after stroke.Acta Pharmacologica Sinica.2023: 1-13. 4. Horie M, Takagane K, Itoh G, et al.Exosomes secreted by ST3GAL5 high cancer cells promote peritoneal dissemination by establishing a pre‐metastatic microenvironment.Molecular Oncology.2023
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相关化合物库

该产品包含在如下化合物库中:
抗阿尔茨海默症化合物库 肿瘤免疫治疗小分子化合物库 FDA 上市药物库 抗病毒库 FDA上市及药典收录分子库 人代谢物化合物库 免疫/炎症分子化合物库 趋化因子抑制剂库 NO PAINS 化合物库 临床期小分子药物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

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: 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 μL,一共给药动物10 只,您使用的配方为5% 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 μL DMSO (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:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步: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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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
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输入分子式,点击计算,可计算出产品的分子量。

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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Maraviroc 376348-65-1 Immunology/Inflammation Microbiology/Virology Proteases/Proteasome HIV Protease CCR CC chemokine receptor inhibit Human immunodeficiency virus UK 427857 HIV Inhibitor Celsentri Selzentry 马拉维若 UK427857 UK-427857 inhibitor

 

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