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

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

目錄號: HY-15601 純度: 99.90%
COA 產品使用指南

Vesatolimod (GS-9620) 是一種有效，選擇性，可口服的 Toll 樣受體7 (TLR7) 激動劑，EC50 值為291 nM。

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Vesatolimod Chemical Structure

Vesatolimod Chemical Structure

CAS No. : 1228585-88-3

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規(guī)格 價格 是否有貨 數量
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
In-stock
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

    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

    • 實驗參考方法

    • 純度 & 產品資料

    • 參考文獻

    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]
    細胞效力
    (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]
    體外研究
    (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.
    體內研究
    (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 號
    性狀

    固體

    顏色

    White to yellow

    中文名稱

    維沙莫德
    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性數據
    細胞實驗： 

    DMSO 中的溶解度 : ≥ 16.67 mg/mL (40.61 mM; 吸濕的 DMSO 對產品的溶解度有顯著影響，請使用新開封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質量 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
    查看完整儲備液配制表

    * 請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    請根據您的 實驗動物和給藥方式 選擇適當的溶解方案。

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實驗結果的可靠性，澄清的儲備液可以根據儲存條件，適當保存；體內實驗的工作液，建議您現用現配，當天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.67 mg/mL (4.07 mM); 澄清溶液

      此方案可獲得 ≥ 1.67 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 16.7 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 1.67 mg/mL (4.07 mM); 懸濁液; 超聲助溶

      此方案可獲得 1.67 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 16.7 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網站選購。 ，Tween 80，均可在 MCE 網站選購。
    計算結果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術支持聯系。
    動物實驗體內工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產品資料

    純度: 99.90%

    參考文獻
    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.
    參考文獻

    完整儲備液配制表

    * 請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

    可選溶劑 濃度 溶劑體積 質量 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.

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    目錄號：
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