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别名 维沙莫德, GS-9620
Vesatolimod (GS-9620) 是一种选择性 Toll 样受体 7 口服激动剂,EC50值为291 nM。


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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 | 库存 | 数量 |
|---|---|---|---|
| 5 mg | ¥ 443 | In Stock | |
| 10 mg | ¥ 875 | In Stock | |
| 25 mg | ¥ 1,774 | In Stock | |
| 50 mg | ¥ 2,460 | In Stock | |
| 100 mg | ¥ 3,997 | In Stock |
Vesatolimod 相关产品
| 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 | Vesatolimod迅速进入细胞,并倾向于定位于内溶酶体区域并从此发出信号。为验证这一假设,采用氚标记的Vesatolimod(3H-Vesatolimod)测量了其在Daudi细胞中的细胞摄取动力学。3H-Vesatolimod的积累动力学快速,大约三十分钟内达到依赖浓度的稳态平衡。测得的3H-Vesatolimod细胞内浓度是用于处理细胞的3H-Vesatolimod外部浓度的5倍。随着3H-Vesatolimod浓度的增加,细胞内3H-Vesatolimod浓度的增加大致成比例[1]。 |
| 体内活性 | 单次口服GS-9620,剂量为0.3和1 mg/kg的未感染黑猩猩,显示剂量和暴露量相关的血清IFN-α、选定细胞因子/趋化因子以及外周血和肝脏中干扰素刺激基因(ISG)的诱导。GS-9620在口服后的最大血浆浓度(Cmax)分别为剂量0.3(n=3)、1 mg/kg(n=3和n=4)时为3.6±3.5、36.8±34.5和55.4±81.0 nM。血清干扰素反应峰值在给药后8小时出现。在0.3和1 mg/kg剂量下,诱导的血清IFN-α平均峰值分别为66和479 pg/mL。GS-9620治疗在0.3 mg/kg剂量下诱导外周血单核细胞(PBMC)中的ISG转录物,包括ISG15、OAS-1、MX1、IP-10(CXCL10)和I-TAC(CXCL11),以及1 mg/kg剂量下诱导PBMC和肝脏中的ISG转录物[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 | 维沙莫德, GS-9620 |
| 分子量 | 410.51 |
| 分子式 | C22H30N6O2 |
| CAS No. | 1228585-88-3 |
| Smiles | CCCCOc1nc(N)c2NC(=O)CN(Cc3cccc(CN4CCCC4)c3)c2n1 |
| 密度 | 1.247 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| 溶解度信息 | DMSO: 4.1 mg/mL (10 mM), Sonication is recommended. | ||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.44 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
DMSO
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