1. Anti-infection Metabolic Enzyme/Protease
  2. HCV Protease HCV SARS-CoV
  3. Telaprevir

Telaprevir  (Synonyms: 特拉匹韦; VX-950)

目录号: HY-10235 纯度: 99.54%
COA 产品使用指南

Telaprevir (VX-950) 是一种有效的选择性的可逆 HCV NS3-4A protease 抑制剂,作用于基因 1型 (H株) NS3 蛋白酶结构域和 NS4A 辅因子肽,Ki 为 7 nM。Telaprevir 抑制 SARS-CoV-2 3CLpro 活性。

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Telaprevir Chemical Structure

Telaprevir Chemical Structure

CAS No. : 402957-28-2

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10 mM * 1 mL in DMSO ¥1234
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5 mg ¥1031
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10 mg ¥1650
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 43 篇科研文献

WB
Proliferation Assay

    Telaprevir purchased from MCE. Usage Cited in: Eur J Med Chem. 2018 Jan 1;143:1053-1065.  [Abstract]

    GS4.3 cells are treated with 7f (20 μM), or Telaprevir (0.5μM), GS-7977 (0.8 μM), BMS-790052 (0.15 μM) or solvent control for 6 days.

    Telaprevir purchased from MCE. Usage Cited in: Sci Rep. 2016 Feb 22;6:21808.  [Abstract]

    While compounds SSO and VX-950 show HCV inhibitory activity in the Group 1 (P < 0.01), SSO-treated viruses display infectivity equal to that of untreated control and negative reference VX-950 in Group 2 (P > 0.05).

    Telaprevir purchased from MCE. Usage Cited in: Antiviral Res. 2015 Dec;124:54-60.  [Abstract]

    Cell lysates at 52 h.p.e are analysed by western blot for NS5A and GAPDH. Both 160 and Telaprevir cause a comparable reduction in NS5A relative to DMSO control.

    Telaprevir purchased from MCE. Usage Cited in: Antimicrob Agents Chemother. 2015 Dec;59(12):7666-7670.  [Abstract]

    Effects of antiviral drugs on cellular uptake of Resorcinol phthalein by BeWo cells. The cells are incubated with 1 μM Resorcinol phthalein in the presence of 100 μM compounds for 10 min at 37°C.

    Telaprevir purchased from MCE. Usage Cited in: Virology. 2014 May;456-457:300-9.  [Abstract]

    Jurkat cells are transfected with plasmids expressing (A) HCV NS3/4A or (B) HPgV NS3/4AB-HA. Telaprevir, EBP 520, and Danoprevir are added at concentrations of 100 µM, 16.6 µM, 2.7 µM, or 0 µM in 0.1% DMSO. Lysates are harvested after 24 h and resolved by immunoblots probed with anti-HCV NS3 (A) or anti-HA (B). The position of HCV NS3/4A (~75kDa), HCV NS3 (~73kDa), NS3/4AB-HA, and NS4B-HA (~30kDa) are indicated. Molecular markers are on the right.

    Telaprevir purchased from MCE. Usage Cited in: Open Virol J. 2014 Mar 7;8:1-8.  [Abstract]

    The PKR activation block is not unique to CypI, DAAs also prevent the IFN-induced PKR activation in HCV-infected cells. JFH-1-infected Huh7.5.1 cells are treated with or without CypI (CsA and alisporivir), DAAs (the HCV NS5A inhibitor BMS-790052 and the HCV protease inhibitor telaprevir) and an HIV-1 inhibitor (reverse transcriptase inhibitor BW1592). Results are representative of 4 independent experiments.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide[1][2][3]. Telaprevir inhibits SARS-CoV-2 3CLpro activity[4].

    IC50 & Target

    Ki: 7 nM (genotype 1 HCV NS3-4A protease)[1]

    体外研究
    (In Vitro)

    Telaprevir (VX-950) 是一种共价、可逆的 NS3-4A 蛋白酶抑制剂,具有缓慢结合和缓慢解离机制。Telaprevir 在酶抑制方面表现出显著不同的动力学,最明显的例子是结合的酶抑制剂复合物的半衰期非常长 (58 分钟)。Telaprevir 与 IFN-α 在抑制 HCV 复制和抑制复制子细胞中出现耐药性方面具有适度协同作用。Telaprevir 以时间和剂量依赖性方式降低 HCV RNA 水平。与 Telaprevir 孵育 24、48、72 和 120 小时后的 IC50 分别确定为 0.574、0.488、0.21 和 0.139 μM,表明抑制作用随时间增加。在 2% FBS 存在下孵育 48 小时的三个独立实验后,Telaprevir 的平均 IC50 确定为 0.354 ± 0.035 μM,平均 IC90 > 为 0.830 ± 0.190 μM[1]。Telaprevir (VX-950) 是一种有效的、选择性的丙型肝炎病毒 (HCV) NS3-4A 丝氨酸蛋白酶拟肽抑制剂,Telaprevir 在基因型 1b HCV 复制子细胞中表现出优异的抗病毒活性 (IC50=354 nM) 和感染基因型 1a HCV 阳性患者血清的人胎儿肝细胞 (IC50=280 nM)[2]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    服用 10 或 25 mg/kg Telaprevir (VX-950) 的小鼠血清 SEAP 活性降低约 5 倍,平均值 (±SEM) 为 18.7±8.3% 或 18.4±5.4%,分别与那些空白组 (100±28%) 相比。这些数据表明,Telaprevir 能够抑制小鼠肝脏中的 HCV NS3-4A 丝氨酸蛋白酶活性,并阻断这些小鼠中 SEAP 的裂解和随后分泌到血液循环中[2]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    679.85

    Formula

    C36H53N7O6

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    特拉普韦;特拉匹韦

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 50 mg/mL (73.55 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.4709 mL 7.3546 mL 14.7091 mL
    5 mM 0.2942 mL 1.4709 mL 2.9418 mL
    查看完整储备液配制表

    * 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
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.68 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.54%

    参考文献
    Cell Assay
    [1]

    Determination of IC50, IC90, CC50 of Telaprevir (VX-950) or IFN-α in HCV replicon cells is performed. Briefly, 1×104 replicon cells per well are plated in 96-well plates. On the following day, replicon cells is incubated at 37°C for the indicated period of time with antiviral agents serially diluted in DMEM plus 2% FBS and 0.5% DMSO. Total cellular RNA is extracted using an RNeasy-96 kit, and the copy number of HCV RNA is determined using a quantitative RT-PCR (QRT-PCR) assay. Each datum point represents the average of five replicates in cell culture. The cytotoxicity of Telaprevir is measured under the same experimental settings using a tetrazolium (MTS)-based cell viability assay. For the cytotoxicity assay with human hepatocyte cell lines, 1×104 parental Huh-7 cells per well or 4×104 HepG2 cells per well are used. To determine cytotoxicity of Telaprevir against resting PBMC, 1×105 cells per well are incubated with Telaprevir in RPMI-1640 medium (no serum) for 48 h, and the cell viability is determined by the MTS-based assay. To determine cytotoxicity of VX-950 against proliferating PBMC, 1×105 cells per well in RPMI-1640 medium are added to a 96-well plate, which is precoated with anti-human CD3 antibody. The cells are incubated with Telaprevir and anti-human CD28 antibody for 72 h at 37°C, and the cell growth is determined by [3H]thymidine update between the 48th and 72nd h[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Mice[2]
    Five groups of 6-week-old SCID mice (6 animals per group) are injected with 109 IFU per mouse of recombinant adenovirus Ad-WT-HCVpro-SEAP through the tail vein. Each group of mice is given two oral administrations of Telaprevir (VX-950) at one of the following doses: 10, 25, 75, 150, or 300 mg/kg. The first Telaprevir dose is given 2 h before the adenovirus injection, and the second dose is given 10 h after injection. An additional group of 10 mice is given vehicle alone. Serum samples are collected 24 h postinjection, and the SEAP activity in each Telaprevir-dosed group is compared to that of the vehicle group. Rat and Dog[2] The intravenous and oral pharmacokinetics of Telaprevir (VX-950) are evaluated in rats and dogs. A group of 3 male Sprague-Dawley rats weighing 250 to 300 g is administered an intravenous bolus dose of 0.95 mg/kg Telaprevir. Serial blood samples are collected in heparinized tubes before dosing and at 0.083, 0.167, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 h after dose administration. A group of 3 male beagle dogs (8 to 12 kg) is administered an intravenous bolus dose of 3.5 mg/kg Telaprevir in 10% ethanol, 40% polyethylene glycol 400, and 50% D5W. Serial blood samples are collected in heparinized tubes before dosing and at 0.083, 0.167, 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, and 24 h after dose administration. For oral studies in rats and dogs, Telaprevir is formulated in polyvinylpyrrolidone (PVP) K-30 plus 2% sodium lauryl sulfate and then dosed as an oral gavage. A group of 3 male Sprague-Dawley rats (250 to 300 g) is dosed orally with 40 mg/kg VX-950, and a group of 4 male beagle dogs (10.9 to 12.0 kg) is administered an oral dose of 9.6 mg/kg VX-950. In both oral studies, blood samples are taken before dosing and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, and 24 h after dose administration. In both intravenous and oral studies, plasma samples are obtained by centrifugation and stored at −70°C until analysis. Samples from the intravenous studies are analyzed by a chiral liquid chromatography followed by tandem mass spectrometry (LC/MS/MS) method, and samples from the oral studies are analyzed using an achiral LC/MS/MS method.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 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
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.4709 mL 7.3546 mL 14.7091 mL 36.7728 mL
    5 mM 0.2942 mL 1.4709 mL 2.9418 mL 7.3546 mL
    10 mM 0.1471 mL 0.7355 mL 1.4709 mL 3.6773 mL
    15 mM 0.0981 mL 0.4903 mL 0.9806 mL 2.4515 mL
    20 mM 0.0735 mL 0.3677 mL 0.7355 mL 1.8386 mL
    25 mM 0.0588 mL 0.2942 mL 0.5884 mL 1.4709 mL
    30 mM 0.0490 mL 0.2452 mL 0.4903 mL 1.2258 mL
    40 mM 0.0368 mL 0.1839 mL 0.3677 mL 0.9193 mL
    50 mM 0.0294 mL 0.1471 mL 0.2942 mL 0.7355 mL
    60 mM 0.0245 mL 0.1226 mL 0.2452 mL 0.6129 mL
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    产品名称:
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    目录号:
    HY-10235
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