| 中文名称: | Vicriviroc maleate 一键复制产品信息 | ||||
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| 英文名称: | Vicriviroc maleate | ||||
| 别名: | 1-[(4,6-二甲基-5-嘧啶基)羰基]-4-[(3S)-4-[(1R)-2-甲氧基-1-[;1-[(4,6-二甲基-5-嘧啶基)羰基]-4-[(3S)-4-[(1R)-2-甲氧基-1-[4-(三氟甲基)苯基]乙基]-3-甲基-1-哌嗪基]-4-甲基哌啶马来酸盐;Vicriviroc Malate 抑制剂 SCH-417690 maleate; SCH-D maleate | ||||
| CAS No: | 599179-03-0 | 分子式: | C28H38F3N5O2.C4H4O4 | 分子量: | 649.7 |
| CAS No: | 599179-03-0 | ||||
| 分子式: | C28H38F3N5O2.C4H4O4 | ||||
| 分子量: | 649.7 | ||||
| MDL: | MFCD09833218 | ||||
基本信息
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产品编号：V10086 |
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产品名称：Vicriviroc maleate |
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CAS: |
599179-03-0 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量： |
649.70 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
134mg/mL (200.68mM) |
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Ethanol |
'134mg/mL |
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Water |
38mg/mL (56.91mM) |
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体内（现配现用） |
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＜1mg/ml表示微溶或不溶。 |
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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。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
1.5392mL |
7.6959mL |
15.3917mL |
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5mM |
0.3078mL |
1.5392mL |
3.0783mL |
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10mM |
0.1539mL |
0.7696mL |
1.5392mL |
生物活性
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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。 |
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靶点/IC50 |
CCR |
HIV |
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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. |
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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. |
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推荐实验方法(仅供参考)
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激酶实验： |
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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。 |
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细胞实验: |
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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. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
