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Vicriviroc maleate

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纯度: 98.37%

货号 T3435Cas号 599179-03-0

别名 维立韦罗马来酸盐, SCH-D (maleate), SCH-417690 (maleate)

Vicriviroc maleate (SCH-417690 (maleate)) 是一种可口服,可透过血脑屏障的 CCR5选择性拮抗剂,同时抑制外周血单核细胞中的 HIV-1 的活性。

Vicriviroc maleate
其他形式的 “Vicriviroc maleate”:
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Vicriviroc maleate

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Rating icon 很棒

纯度: 98.37%

货号 T3435 别名 维立韦罗马来酸盐, SCH-D (maleate), SCH-417690 (maleate)Cas号 599179-03-0

Vicriviroc maleate (SCH-417690 (maleate)) 是一种可口服,可透过血脑屏障的 CCR5选择性拮抗剂,同时抑制外周血单核细胞中的 HIV-1 的活性。

规格价格库存数量
1 mg
¥ 343
现货
5 mg
¥ 828
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10 mg
¥ 1,180
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25 mg
¥ 2,250
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50 mg
¥ 3,160
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100 mg
¥ 4,420
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200 mg
¥ 5,960
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1 mL x 10 mM (in DMSO)
¥ 1,150
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产品介绍


Vicriviroc maleate AI Summary
Vicriviroc maleate exhibits diverse bioactivities, notably including antiviral properties and interactions with GPCR targets. At a concentration of 10 µM, it shows an inhibition of 5.07% on SARS-CoV-2 induced cytotoxicity in Caco-2 cells and modest inhibitory activity against the SARS-CoV-2 3CL-Pro protease, with a 2.58% inhibition at 20 µM as determined by a FRET-based assay using a peptide substrate. However, the compound demonstrates a considerably lower inhibition percentage (-0.04%) on the virus-induced cytotoxicity in VERO-6 cells under similar conditions. In terms of cellular effects, Vicriviroc maleate influences cell viability in a context-dependent manner across different cell types, such as HEK293T, U2OS, and human fibroblasts, indicating both stimulating and inhibiting effects on growth rates. It also affects the thermal stability of various protein domains, increasing stability in some (e.g., M1-L298, M1-S360) while decreasing it in others (e.g., N44-E168, M626-G740). Additionally, it has been identified as a GPCR beta-arrestin recruiter, impacting targets including ADGRF1, S1PR1, APLNR, C5AR1, and others, demonstrating both stimulatory and inhibitory effects at a very low concentration (0.00001)..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Vicriviroc maleate (SCH-417690 (maleate))(Sch-417690) is a piperazine-based CCR5 receptor antagonist with activity against human immunodeficiency virus. The IC50 value is 0.91 nM in clinical development for the treatment of HIV-1.
靶点活性
CCR5 receptor:0.91 nM, CCR5 receptor:2.5 nM (Ki), HIV-1 (301657):1.8 nM (IC90, in PBMC cells), HIV-1 (RU 570):10 nM (IC90, in PBMC cells), HIV-1 (JrFL):3.3 nM (IC90, in PBMC cells), HIV-1 (JV1083):4.9 nM (IC90, in PBMC cells), HIV-1 (ADA-M):2.8 nM (IC90, in PBMC cells)
别名维立韦罗马来酸盐, SCH-D (maleate), SCH-417690 (maleate)
化学信息
分子量649.7
分子式C32H42F3N5O6
CAS No.599179-03-0
SmilesOC(=O)\C=C/C(O)=O.COC[C@H](N1CCN(C[C@@H]1C)C1(C)CCN(CC1)C(=O)c1c(C)ncnc1C)c1ccc(cc1)C(F)(F)F
密度no data available
颜色White
物理性状Solid
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
DMSO: 50 mg/mL (76.96 mM), Sonication is recommended.
H2O: 25 mg/mL (38.48 mM), Sonication and heating are recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.08 mM), Sonication is recommended.
请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。
溶液配制表
H2O/DMSO
1mg5mg10mg50mg
1 mM1.5392 mL7.6959 mL15.3917 mL76.9586 mL
5 mM0.3078 mL1.5392 mL3.0783 mL15.3917 mL
10 mM0.1539 mL0.7696 mL1.5392 mL7.6959 mL
20 mM0.0770 mL0.3848 mL0.7696 mL3.8479 mL
DMSO
1mg5mg10mg50mg
50 mM0.0308 mL0.1539 mL0.3078 mL1.5392 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20g,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%Saline/PBS/ddH2O, 那么您的工作液浓度为2mg/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 50μLTween80, 混匀澄清,再加 600μLSaline/PBS/ddH2OTargetMol | 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。

方案所需的各类助溶剂如: DMSOPEG300 / PEG400Tween 80SBE-β-CD玉米油 等, 均可在TargetMol网站点击购买。
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
% Saline/PBS/ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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