Vesatolimod (GS-9620)

Catalog No.S7221 Batch:S722101

Technical Data

Formula

C₂₂H₃₀N₆O₂

Molecular Weight

410.51

CAS No.

1228585-88-3

Solubility (25°C)*

In vitro

4-Methylpyridine (warmed with 50ºC water bath)

12 mg/mL (29.23 mM)

DMSO (warmed with 50ºC water bath)

8.8 mg/mL (21.43 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

0.44mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 8.8 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:^{^[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 Study:^{^[1]}	Animal Models chimpanzees Dosages 1 mg/kg and 2 mg/kg Administration oral administration

Cell Assay:^{^[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 Study:^{^[1]}

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

References

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

β-catenin regulates HIV latency and modulates HIV reactivation [ PLoS Pathog, 2022, 18(3):e1010354]	PubMed: 35255110
Determination of motolimod concentration in rat plasma by liquid chromatography-tandem mass spectrometry and its application in a pharmacokinetic study. [ J Pharm Biomed Anal, 2020, 179:112987]	PubMed: 31761376
Activation of type I interferon antiviral response in human neural stem cells. [ Stem Cell Res Ther, 2019, 10(1):387]	PubMed: 31843025
TLR7/8-agonist-loaded Nanoparticles Promote the Polarization of Tumour-Associated Macrophages to Enhance Cancer Immunotherapy [ Nat Biomed Eng, 2018, 2(8):578-588]	PubMed: 31015631
3D microfluidic liver cultures as a physiological preclinical tool for hepatitis B virus infection. [ Nat Commun, 2018, 9(1):682]	PubMed: 29445209
Structural Analyses of Toll-like Receptor 7 Reveal Detailed RNA Sequence Specificity and Recognition Mechanism of Agonistic Ligands. [ Cell Rep, 2018, 25(12):3371-3381]	PubMed: 30566863

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.