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- 详细信息
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Vesatolimod
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1228585-88-3
- 规格：
100mg/50mg/25mg/10mg/1mg/5mg
| 规格： | 100mg | 产品价格： | ￥4830.0 |
|---|---|---|---|
| 规格： | 50mg | 产品价格： | ￥2960.0 |
| 规格： | 25mg | 产品价格： | ￥2080.0 |
| 规格： | 10mg | 产品价格： | ￥1040.0 |
| 规格： | 1mg | 产品价格： | ￥240.0 |
| 规格： | 5mg | 产品价格： | ￥540.0 |
是Toll样受体7（TLR-7）的新型有效，选择性的小分子激动剂
| 基本信息 | |
| CAS | No.1228585-88-3 |
| 中文名称 | 维沙莫德 |
| 英文名称 | Vesatolimod |
| 别名 | GS-9620 |
| 分子式 | C22H30N6O2 |
| 分子量 | 410.51 |
| 溶解性 | Soluble in DMSO ≥1mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | White to light yellow Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD25372045 |
| SMILES | O=C1NC2=C(N)N=C(OCCCC)N=C2N(CC3=CC=CC(CN4CCCC4)=C3)C1 |
| 靶点 | Toll-like Receptor (TLR) |
| 通路 | Immunology & Inflammation |
| 背景说明 | Vesatolimod是Toll样受体7(TLR-7)的新型有效,选择性的小分子激动剂。 |
| 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.[1-3] |
| IC50 | EC50: 291 nM (TLR7)， 9 μM (TLR8)[3] |
| 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]. |
| 细胞实验 | 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]. |
| 细胞实验 | 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]. |
| 动物实验 | 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. |
| 数据来源文献 | [1]. Rebbapragada I， et al. Molecular Determinants of GS-9620-Dependent TLR7 Activation. PLoS One. 2016 Jan 19;11(1):e0146835. [2]. Lanford RE， et al. GS-9620， an Oral Agonist of Toll-Like Receptor-7， Induces Prolonged Suppression of Hepatitis B Virus in Chronically Infected Chimpanzees. Gastroenterology. 2013 Feb 13. pii: S0016-5085(13)00169-8. [3]. D Tumas， et al. Preclinical Characterization of GS-9620， A Potent and Selective Oral TLR7 Agonist. |
| 单位 | 瓶 |
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IV0740 维沙莫德 免疫学/炎症 索莱宝
￥240 - 4830
