Vesatolimod (GS-9620)

Catalog No.S7221

For research use only.

Vesatolimod (GS-9620) is a potent and selective orally active small molecule agonist of Toll-like receptor 7.

Vesatolimod (GS-9620) Chemical Structure

CAS No. 1228585-88-3

Selleck's Vesatolimod (GS-9620) has been cited by 6 Publications

Purity & Quality Control

Choose Selective TLR Inhibitors

Biological Activity

Description Vesatolimod (GS-9620) is a potent and selective orally active small molecule agonist of Toll-like receptor 7.
Targets
TLR7 [1]
In vitro

GS-9620 potently inhibited viral replication in peripheral blood mononuclear cells(PBMCs), particularly when added 24 to 48 hours prior to HIV infection (EC50= 27 nM). Depletion of pDCs, but not other immune cell subsets from PBMC cultures, suppressed GS-9620 antiviral activity[2].

In vivo Short-term oral administration of GS-9620 provides long-term suppression of serum and liver HBV DNA. GS-9620 administration induces production of IFN-α and other cytokines and chemokines, and activates ISGs, natural killer cells, and lymphocyte subsets. Its treatment reduces viral DNA, Serum levels of HB surface antigen, HB e antigen and numbers of HBV antigen-positive hepatocytes while hepatocyte apoptosis increases[1]. Currently, GS-9620 is under clinical evaluation for treating chronic HBV infection and for reducing latent reservoirs in virally-suppressed HIV-infected patients[2].

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: Human PBMCs
  • Concentrations: serial dilutions
  • Incubation Time: 5 days
  • Method:

    Uninfected PBMCs from individual donors are first activated in bulk using PHA and IL-2 at 37°C for 48 hours and then seeded into 96-well plates at a density of 2 x 105 cells per well before being dosed in triplicate with 4-fold serial dilutions of compounds prepared in RPMI cell culture medium. Cells are incubated in a 5% CO2 incubator at 37°C for a period of 5 days. At the end of the assay,
    cell viability is assessed.

Animal Research:

[1]

  • Animal Models: chimpanzees
  • Dosages: 1 mg/kg and 2 mg/kg
  • Administration: oral administration

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 410.51
Formula

C22H30N6O2

CAS No. 1228585-88-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCCOC1=NC(=C2C(=N1)N(CC(=O)N2)CC3=CC=CC(=C3)CN4CCCC4)N

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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