Shopping Cart
- Remove All
![TargetMol](https://www.targetmol.com/storage/error/oops.webp)
Your shopping cart is currently empty
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $45 | In Stock | |
10 mg | $86 | In Stock | |
25 mg | $173 | In Stock | |
50 mg | $246 | In Stock | |
100 mg | $397 | In Stock | |
1 mL x 10 mM (in DMSO) | $50 | In Stock |
Description | Vesatolimod (GS-9620) is an effective and specific orally active agonist of Toll-like receptor 7. |
In vitro | 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]. |
In vivo | Administering single oral doses of GS-9620 at 0.3 and 1 mg/kg to uninfected chimpanzees resulted in a dose-dependent increase in serum interferon alpha (IFN-α), various cytokines/chemokines, and activation of interferon-stimulated genes (ISG) in both peripheral blood and liver tissues. Specifically, GS-9620 reached peak plasma concentrations (Cmax) of 3.6±3.5 nM at 0.3 mg/kg (n=3), 36.8±34.5 nM at 1 mg/kg (n=3), and 55.4±81.0 nM at 1 mg/kg (n=4), respectively, with peak serum interferon responses recorded 8 hours after dosing. The induced peak serum levels of IFN-α were measured at 66 pg/mL for the 0.3 mg/kg dose and 479 pg/mL for the 1 mg/kg dose. Treatment with GS-9620 at these doses also elevated ISG transcripts, specifically ISG15, OAS-1, MX1, IP-10 (CXCL10), and I-TAC (CXCL11), in peripheral blood mononuclear cells (PBMC) at the lower dose and in both PBMC and liver at the higher dose. |
Kinase Assay | Biochemical assays: Biochemical assays are performed by a broad-coverage, TR-FRET-based kinase binding assay platform. |
Cell Research | 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]. |
Alias | GS-9620 |
Molecular Weight | 410.51 |
Formula | C22H30N6O2 |
Cas No. | 1228585-88-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||
Solubility Information | DMSO: 4.1 mg/mL (10 mM) ![]() | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
DMSO
|
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.