2. Anti-infection
  3. HCV SARS-CoV
  4. Ledipasvir

Ledipasvir  (Synonyms: 雷迪帕韦; GS-5885)

目录号: HY-15602 纯度: 99.68%
COA 产品使用指南

摩尔计算器

Ledipasvir (GS-5885) 是一种有效的 HCV NS5A 抑制剂，能够抑制 GT1a 和 GT1b 复制子，EC50 值分别为 34 pM 和 4 pM。Ledipasvir 也是 SARS-CoV 3CLpro 的抑制剂，IC50 为 1.62 μM。

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Ledipasvir Chemical Structure

Ledipasvir Chemical Structure

CAS No. : 1256388-51-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1956
In-stock
2 mg ￥800
In-stock
5 mg ￥1200
In-stock
10 mg ￥2000
In-stock
25 mg ￥3492
In-stock
50 mg ￥5238
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Ledipasvir:

Ledipasvir 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 32 篇科研文献

WB

    Ledipasvir purchased from MCE. Usage Cited in: Antimicrob Agents Chemother. 2015 Jun;59(6):3482-92.  [Abstract]

    Assessment of HCV inhibition by DAAs from 3 classes using Western blot analysis. Jc1/Gluc2A virus-infected Huh-7.5.1 cells are treated with DMSO or the HCV inhibitors at concentrations of 100× EC50 (DCV, 3.2 nM; LDV, 3 μM; DNV, 0.32 μM; SOF, 20 μM). Cell lysates are harvested at 8 hpt (C and D) or at 24 hpt (A and B) and blotted for NS5A (A and C) or core (B and D). Data are normalized to GAPDH and quantified as relative fold change with respect to DMSO.

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM[3].

    IC50 & Target

    EC50: 34 pM (GT1a), 4 pM (GT1b)[1]
    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    Huh-7 EC50
    210 pM
    Compound: 39, GS-5885, ledipasvir
    Antiviral activity against HCV genotype 1a H77 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay in presence of 10% BSA
    Antiviral activity against HCV genotype 1a H77 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay in presence of 10% BSA
    		[PMID: 24320933]
    Huh-7 EC50
    210 pM
    Compound: 39, GS-5885, ledipasvir
    Antiviral activity against HCV genotype 1a H77 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay in presence of human serum
    Antiviral activity against HCV genotype 1a H77 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay in presence of human serum
    		[PMID: 24320933]
    Huh-7 EC50
    27 pM
    Compound: 39, GS-5885, ledipasvir
    Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay in presence of human serum
    Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay in presence of human serum
    		[PMID: 24320933]
    Huh-7 EC50
    27 pM
    Compound: 39, GS-5885, ledipasvir
    Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay in presence of 10% BSA
    Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay in presence of 10% BSA
    		[PMID: 24320933]
    Huh-7 EC50
    31 pM
    Compound: 39, GS-5885, ledipasvir
    Antiviral activity against HCV genotype 1a H77 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay
    Antiviral activity against HCV genotype 1a H77 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay
    		[PMID: 24320933]
    Huh-7 EC50
    4 pM
    Compound: 39, GS-5885, ledipasvir
    Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay
    Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay
    		[PMID: 24320933]
    体外研究
    (In Vitro)

    Ledipasvir 对基因型 1a 和 1b 的 EC50 值分别为 31 pM 和 4 pM；经蛋白质调整后的 EC50 值分别为 210 pM（基因型1a）和27 pM（基因型1b）。内在 EC50 值为 39 时，基因型 1a 为 310 fM，基因型 1b 为 40 fM。Ledipasvir 在人血清以及含有10%牛血清白蛋白（BSA）的细胞培养基中均高度与蛋白质结合[1]。
    Ledipasvir 对 JFH/3a-NS5A 复制子的 EC50 值为 141 nM[2]。

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

    Ledipasvir 相关抗体:
    体内研究
    (In Vivo)

    Ledipasvir不仅因其高效的复制子活性而引人注目，还因为其低清除率、良好的生物利用度以及在大鼠、狗和猴子体内的长半衰期，同时预测的人体清除率也较低。Ledipasvir的药代动力学已在大鼠和狗身上进行了测量。Ledipasvir在血浆中具有良好的半衰期（大鼠为1.83 ± 0.22小时，狗为2.63 ± 0.18小时），系统清除率低，且分布容积（Vss）适中，超过了总体水体积[1]。

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

    889.00

    Formula

    C49H54F2N8O6
    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    中文名称

    雷迪帕韦；来地帕韦
    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
    细胞实验： 

    DMSO 中的溶解度 : 50 mg/mL (56.24 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.1249 mL 5.6243 mL 11.2486 mL
    5 mM 0.2250 mL 1.1249 mL 2.2497 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

    动物实验：

    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (2.81 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。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

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

      Solubility: ≥ 2.5 mg/mL (2.81 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。

      以 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

    只
    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: 99.68%

    COA (200 KB) LCMS (93 KB)

    产品使用指南 (1538 KB)
    参考文献
    Animal Administration
    [1]

    Rats, Dogs and Monkeys[1]
    Pharmacokinetic studies are performed in male naı̈ve Sprague-Dawley(SD) rats, non-naive beagle dogs, and cynomolgus monkeys (three animals per dosing route). Intravenous (IV) administration is dosed via infusion over 30 min in a vehicle containing 5% ethanol, 20% PEG400, and 75% water (pH adjusted to 3.0 with HCl). Oral dosing is administered by gavage in a vehicle containing 5% ethanol, 45% PEG 400, and 50% of 50 mM citrate buffer, pH 3. Blood samples are collected over a 24 h period postdose into Vacutainer tubes containing EDTA-K2. Plasma was isolated, and the concentration of the test compound in plasma was determined with LC/MS/MS after protein precipitation with acetonitrile.

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

    Ledipasvir 相关分类

    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 1.1249 mL 5.6243 mL 11.2486 mL 28.1215 mL
    5 mM 0.2250 mL 1.1249 mL 2.2497 mL 5.6243 mL
    10 mM 0.1125 mL 0.5624 mL 1.1249 mL 2.8121 mL
    15 mM 0.0750 mL 0.3750 mL 0.7499 mL 1.8748 mL
    20 mM 0.0562 mL 0.2812 mL 0.5624 mL 1.4061 mL
    25 mM 0.0450 mL 0.2250 mL 0.4499 mL 1.1249 mL
    30 mM 0.0375 mL 0.1875 mL 0.3750 mL 0.9374 mL
    40 mM 0.0281 mL 0.1406 mL 0.2812 mL 0.7030 mL
    50 mM 0.0225 mL 0.1125 mL 0.2250 mL 0.5624 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Ledipasvir1256388-51-8GS-5885雷迪帕韦来地帕韦GS5885GS 5885HCVSARS-CoVHepatitis C virusSARS coronavirusInhibitorinhibitorinhibit

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