2. Immunology/Inflammation Apoptosis Anti-infection
  3. Toll-like Receptor (TLR) Apoptosis HBV HCV HIV
  4. Vesatolimod

Vesatolimod  (Synonyms: 维沙莫德; GS-9620)

目录号: HY-15601 纯度: 99.90%
COA 产品使用指南

摩尔计算器

Vesatolimod (GS-9620) 是一种有效，选择性，可口服的 Toll 样受体7 (TLR7) 激动剂，EC50 值为291 nM。

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Vesatolimod Chemical Structure

Vesatolimod Chemical Structure

CAS No. : 1228585-88-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥605
In-stock
1 mg ￥250
In-stock
5 mg ￥550
In-stock
10 mg ￥1050
In-stock
25 mg ￥2090
In-stock
50 mg ￥2970
In-stock
100 mg ￥4840
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200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Vesatolimod 相关抗体

Top Publications Citing Use of Products

    Vesatolimod purchased from MCE. Usage Cited in: Antiviral Res. 2018 May;153:39-48.  [Abstract]

    The expression of proteins is determined by western blot, which are up-regulated by EV71 infection and repressed by GS-9620 treatment.

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    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Vesatolimod (GS-9620) is a potent, selective and orally active agonist of Toll-Like Receptor (TLR7) with an EC50 of 291 nM.

    IC50 & Target

    EC50: 291 nM (TLR7), 9 μM (TLR8)[3]
    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HEK293 EC50
    290 nM
    Compound: 5, GS-9620
    Agonist activity at human TLR7 expressed in HEK293 cells by reporter based assay
    Agonist activity at human TLR7 expressed in HEK293 cells by reporter based assay
    		[PMID: 23961878]
    HEK293 EC50
    9 μM
    Compound: 5, GS-9620
    Agonist activity at human TLR8 expressed in HEK293 cells by reporter based assay
    Agonist activity at human TLR8 expressed in HEK293 cells by reporter based assay
    		[PMID: 23961878]
    体外研究
    (In Vitro)

    Vesatolimod (GS-9620) rapidly internalizes into cells and preferentially localizes to and signals from endo-lysosomal compartments. To test this hypothesis, the kinetics of cellular uptake of the compound in Daudi cells using tritiated Vesatolimod (3H-GS-9620) is measured. The kinetics of 3H-GS-9620 accumulation is rapid, reaching concentration-dependent steady-state equilibrium in approximately thirty minutes. Measured intracellular concentration of 3H-Vesatolimod is 5-fold higher than the extracellular concentration of 3H-GS-9620 used to treat cells. Increases in intracellular 3H-Vesatolimod concentrations are roughly proportional with increasing concentrations of 3H-GS-9620[1].

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

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

    Single oral doses of Vesatolimod (GS-9620) at 0.3 and 1 mg/kg in uninfected chimpanzees demonstrates a dose- and exposure-related induction of serum IFN-α, select cytokines/chemokines, and IFN-stimulated genes (ISG) in the peripheral blood and liver. Following oral administration at 0.3 (n=3), and 1 mg/kg (n=3 and n=4), Vesatolimod (GS-9620) Cmax is 3.6±3.5, 36.8±34.5, and 55.4±81.0 nM, respectively. Peak serum IFN responses occur at 8 h post-dose. The mean peak levels of induced serum IFN-α are 66 and 479 pg/mL at doses of 0.3 and 1 mg/kg, respectively. Vesatolimod (GS-9620) treatment induces ISG transcripts including ISG15, OAS-1, MX1, IP-10 (CXCL10), and I-TAC (CXCL11) in peripheral blood mononuclear cells (PBMC) at 0.3 mg/kg and in both PBMC and the liver at 1 mg/kg[2].

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

    410.51

    Formula

    C22H30N6O2
    CAS 号
    性状

    固体

    颜色

    White to yellow

    中文名称

    维沙莫德
    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 6 months
    -20°C 1 month
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 16.67 mg/mL (40.61 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 2.4360 mL 12.1800 mL 24.3599 mL
    5 mM 0.4872 mL 2.4360 mL 4.8720 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    • 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: ≥ 1.67 mg/mL (4.07 mM); 澄清溶液

      此方案可获得 ≥ 1.67 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 16.7 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% (20% SBE-β-CD in Saline)

      Solubility: 1.67 mg/mL (4.07 mM); 悬浊液; 超声助溶

      此方案可获得 1.67 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
    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: 99.90%

    COA (268 KB) LCMS (90 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [1]

    Daudi cells are incubated for indicated times with varying concentrations [3H]Vesatolimod (GS-9620) (0.7μCi/mL). Cell associated radioactivity is extracted with ice cold 80% ethanol and measured using liquid scintillation counting. The total amount of Vesatolimod in cells is calculated from a calibration curve for Vesatolimod (GS-9620) mass versus radioactivity. Cell volume is measured[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Chimpanzee[2]
    Chimpanzees are used. The trial design includes 4 weeks of pre-study evaluation (Day-28, -13 and just prior to first dose) and two cycles of oral Vesatolimod (GS-9620) treatment every other day three times per week for 4 weeks with one cycle at 1 mg/kg, and, after a one week rest, a second cycle at 2 mg/kg. Animals are also intensely monitored for 14 weeks after treatment to assess tolerability and durability of response.

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

    Vesatolimod 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4360 mL 12.1800 mL 24.3599 mL 60.8999 mL
    5 mM 0.4872 mL 2.4360 mL 4.8720 mL 12.1800 mL
    10 mM 0.2436 mL 1.2180 mL 2.4360 mL 6.0900 mL
    15 mM 0.1624 mL 0.8120 mL 1.6240 mL 4.0600 mL
    20 mM 0.1218 mL 0.6090 mL 1.2180 mL 3.0450 mL
    25 mM 0.0974 mL 0.4872 mL 0.9744 mL 2.4360 mL
    30 mM 0.0812 mL 0.4060 mL 0.8120 mL 2.0300 mL
    40 mM 0.0609 mL 0.3045 mL 0.6090 mL 1.5225 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:

    Vesatolimod1228585-88-3GS-9620维沙莫德GS9620GS 9620Toll-like Receptor (TLR)ApoptosisHBVHCVHIVHepatitis B virusHepatitis C virusHuman immunodeficiency virusInhibitorinhibitorinhibit

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