Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Vesatolimod (GS-9620) 是一种选择性 Toll 样受体 7 口服激动剂,EC50值为291 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 443 | 现货 | ||
10 mg | ¥ 875 | 现货 | ||
25 mg | ¥ 1,774 | 现货 | ||
50 mg | ¥ 2,460 | 现货 | ||
100 mg | ¥ 3,997 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 491 | 现货 |
产品描述 | Vesatolimod (GS-9620) is an effective and specific orally active agonist of Toll-like receptor 7. |
靶点活性 | TLR7:291 nM(EC50) |
体外活性 | 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 GS-9620 (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-GS-9620 is 5-fold higher than the extracellular concentration of 3H-GS-9620 used to treat cells. Increases in intracellular 3H-GS-9620 concentrations are roughly proportional with increasing concentrations of 3H-GS-9620[1]. |
体内活性 | Single oral doses of 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 interferon-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), GS-9620 Cmax is 3.6±3.5, 36.8±34.5, and 55.4±81.0 nM, respectively. Peak serum interferon 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. 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]. |
激酶实验 | Biochemical assays: Biochemical assays are performed by a broad-coverage, TR-FRET-based kinase binding assay platform. |
细胞实验 | GS-9620 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. Daudi cells are incubated for indicated times with varying concentrations [3H]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 GS-9620 in cells is calculated from a calibration curve for GS-9620 mass versus radioactivity. Cell volume is measured[1]. |
别名 | GS-9620, 维沙莫德 |
分子量 | 410.51 |
分子式 | C22H30N6O2 |
CAS No. | 1228585-88-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 4.1 mg/mL (10 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.436 mL | 12.18 mL | 24.3599 mL | 60.8999 mL |
5 mM | 0.4872 mL | 2.436 mL | 4.872 mL | 12.18 mL | |
10 mM | 0.2436 mL | 1.218 mL | 2.436 mL | 6.09 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (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:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Vesatolimod 1228585-88-3 Apoptosis Immunology/Inflammation Microbiology/Virology Proteases/Proteasome HIV Protease HCV Protease HBV TLR Hepatitis B virus HCV inhibit Human immunodeficiency virus GS9620 Inhibitor Hepatitis C virus GS-9620 HIV GS 9620 维沙莫德 Toll-like Receptor (TLR) inhibitor