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Vicriviroc maleate  ≥98%

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包装规格：1mg 5mg in glass bottle
溶解性：溶于DMSO（50 mg/mL 超声)
产品描述：基本信息 产品编号：V10086 产品名称：Vicriviroc maleate CAS: 599179-03-0   储存条件 粉末 -20℃ 四年     分子式： C28H38F3N5O2.C4H4O4 溶于液体 -80℃ 六个月 分子量： 649.70 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 134mg/mL (200.68mM) Ethanol '134mg/mL Water 38mg/mL (56.91mM) 体内（现配现用）     ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.5392mL 7.6959mL 15.3917mL 5mM 0.3078mL 1.5392mL 3.0783mL 10mM 0.1539mL 0.7696mL 1.5392mL   生物活性 产品描述 一种有效，选择性，可口服，可透过血脑屏障的 CCR5 拮抗剂，Ki 值为 2.5nM，同时抑制外周血单核细胞中的 HIV-1 的活性。 靶点/IC50 CCR HIV   体外研究 Vicriviroc maleate (SCH-417690 maleate;SCH-D maleate) is a potent,selective and oral bioavailable inhibitor of CCR5,with a Ki of 2.5nM,and also inhibits HIV-1 in PBMC cells,with IC90s of 3.3 (JrFL),2.8 (ADA-M),1.8 (301657),4.9 (JV1083) and 10nM (RU 570).In addition,Vicriviroc maleate shows a mean IC50 and IC90 of 0.45nM and 4nM for a panel of HIV isolates,and has weak activity against hERG activity (IC50,5.8μM).Vicriviroc maleate inhibits chemotactic response to MIP-1αwith IC50 values below 1nM,and suppresses RANTES-induced signaling with a mean IC50 of 4.2±1.3nM.Vicriviroc maleate potently suppresses all the viral isolates tested,with geometric mean EC50s of 0.04-2.3nM and IC90s of 0.45-18nM. 体内研究 Vicriviroc maleate (SCH-417690 maleate;SCH-D maleate;10mg/kg) has good oral availablity in rats and monkeys,with no acute CNS or GI effects in rats.   推荐实验方法(仅供参考) 激酶实验： 趋化实验 使用浓度不断增高的Vicriviroc 在趋化buffer(含1% FBS 和0.1μg/mL小鼠 IL-3的RPMI培养基)中在 37oC下预处理Ba/F3-CCR5细胞。含Vicriviroc 和 MIP-1α(0.3nM),MIP-1β (0.3nM),或RANTES (0.3nM)的趋化 buffer置于 5-μm ChemoTx 实验板的孔底，过滤装置置于孔中。吸取Vicriviroc 预处理的Ba/F3-CCR5 细胞(25μL)到过滤器上，然后实验板在37oC下温育2小时。未迁移的细胞从过滤器中擦去，实验板离心得到迁移的细胞。细胞然后转移到 Microlite 1+Flatbottom Microtiter 板上，使用发光细胞活力检测试剂盒定量测量。使用 GraphPad Prism 软件测定Vicriviroc 作用的IC50值。   细胞实验:   Ficoll-purified peripheral blood mononuclear cells (PBMCs) are stimulated in vitro with phytohemagglutinin (PHA) (5μg/mL) and interleukin-2 (IL-2) (50U/mL) for 3 to 7 days.The cells are resuspended at 4×106/mL in complete medium (RPMI,10% fetal bovine serum [FBS],50U/mL IL-2),seeded into 96-well plates (2×105/well),incubated with an equal volume of culture medium containing compound (Vicriviroc) for 1 h at 37℃,and infected in triplicate with 25 to 100 50% tissue culture infectious doses (TCID50) per well of viral inoculum for 3 to 4h.Cells are washed twice in phosphate-buffered saline (PBS) to remove residual virus and are cultured with compound for 4 to 6 days.HIV-1 replication is quantified by measurement of extracellular p24 antigen in the supernatants by enzyme-linked immunosorbent assay.The 50% effective concentrations (EC50s) and EC90s for each virus are determined using Graphpad PRISM software.
保存条件：-20℃

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