S81251 |
GS-9620 |
| 源叶(MedMol) | 98% |
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- 产品描述： Vesatolimod (GS-9620) is a potent, selective and orally active agonist of Toll-Like Receptor (TLR7) with an EC50 of 291 nM.
- 靶点： EC50: 291 nM (TLR7), 9 μM (TLR8)
- 体内研究： 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
- 参考文献：
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.
- 溶解性： DMSO : ≥ 16.67 mg/mL (40.61 mM)
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.436 ml 12.18 ml 24.36 ml 5 mM 0.487 ml 2.436 ml 4.872 ml 10 mM 0.244 ml 1.218 ml 2.436 ml 50 mM 0.049 ml 0.244 ml 0.487 ml
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
