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Vesatolimod

Catalog No. T6846 CAS 1228585-88-3

Synonyms: GS-9620

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Vesatolimod, CAS 1228585-88-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 45.00
10 mg	In stock	$ 86.00
25 mg	In stock	$ 173.00
50 mg	In stock	$ 246.00
100 mg	In stock	$ 397.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.92%

Purity: 98.47%

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Description	Vesatolimod (GS-9620) is an effective and specific orally active agonist of Toll-like receptor 7.
Targets&IC50	TLR7:291 nM(EC50)
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].

Synonyms	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), Sonication is recommended.

References and Literature

1. Rebbapragada I, et al. Molecular Determinants of GS-9620-Dependent TLR7 Activation. PLoS One. 2016 Jan 19;11(1):e20146835. 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.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Bioactive Compounds Library Max Immunology/Inflammation Compound Library Apoptosis Compound Library Anti-Infection Compound Library Anti-COVID-19 Compound Library Target-Focused Phenotypic Screening Library Bioactive Compound Library Immuno-Oncology Compound Library HIF-1 Signaling Pathway Compound Library

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Keywords

Vesatolimod 1228585-88-3 Apoptosis Immunology/Inflammation Microbiology/Virology Proteases/Proteasome HIV Protease HCV Protease HBV TLR Hepatitis B virus HCV inhibit Human immunodeficiency virus GS9620 Inhibitor Hepatitis C virus GS-9620 HIV GS 9620 Toll-like Receptor (TLR) inhibitor

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