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Vesatolimod
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Vesatolimod图片
CAS NO:1228585-88-3
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
维沙莫德
GS-9620
产品介绍
Vesatolimod 是一种选择性 Toll 样受体 7 口服激动剂,EC50值为291 nM。

产品描述

GS-9620 is an effective and specific orally active agonist of Toll-like receptor 7.

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].

Cas No.

1228585-88-3

分子式

C22H30N6O2

分子量

410.522

别名

维沙莫德;GS-9620

储存和溶解度

DMSO:10mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years