1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)
  3. Vesatolimod

Vesatolimod (Synonyms: GS-9620)

Cat. No.: HY-15601 Purity: 98.80%
Handling Instructions

Vesatolimod (GS-9620) is a potent, selective and orally active agonist of Toll-Like Receptor (TLR7) with an EC50 of 291 nM.

For research use only. We do not sell to patients.

Vesatolimod Chemical Structure

Vesatolimod Chemical Structure

CAS No. : 1228585-88-3

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 121 In-stock
Estimated Time of Arrival: December 31
5 mg USD 110 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 650 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Top Publications Citing Use of Products

    Vesatolimod purchased from MCE. Usage Cited in: Antiviral Res. 2018 Feb 6;153:39-48.

    The expression of proteins is determined by western blot, which are up-regulated by EV71 infection and repressed by GS-9620 treatment.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Vesatolimod (GS-9620) is a potent, selective and orally active agonist of Toll-Like Receptor (TLR7) with an EC50 of 291 nM.

    IC50 & Target

    EC50: 291 nM (TLR7), 9 μM (TLR8)[3]

    In Vitro

    Vesatolimod (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 Vesatolimod (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-Vesatolimod is 5-fold higher than the extracellular concentration of 3H-GS-9620 used to treat cells. Increases in intracellular 3H-Vesatolimod concentrations are roughly proportional with increasing concentrations of 3H-GS-9620[1].

    In Vivo

    Single oral doses of Vesatolimod (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), Vesatolimod (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. Vesatolimod (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].

    Clinical Trial
    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 4.8 mg/mL (11.69 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4360 mL 12.1800 mL 24.3599 mL
    5 mM 0.4872 mL 2.4360 mL 4.8720 mL
    10 mM 0.2436 mL 1.2180 mL 2.4360 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [1]

    Daudi cells are incubated for indicated times with varying concentrations [3H]Vesatolimod (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 Vesatolimod in cells is calculated from a calibration curve for Vesatolimod (GS-9620) mass versus radioactivity. Cell volume is measured[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Chimpanzee[2]
    Chimpanzees are used. The trial design includes 4 weeks of pre-study evaluation (Day-28, -13 and just prior to first dose) and two cycles of oral Vesatolimod (GS-9620) treatment every other day three times per week for 4 weeks with one cycle at 1 mg/kg, and, after a one week rest, a second cycle at 2 mg/kg. Animals are also intensely monitored for 14 weeks after treatment to assess tolerability and durability of response.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    410.51

    Formula

    C₂₂H₃₀N₆O₂

    CAS No.

    1228585-88-3

    SMILES

    O=C1NC2=C(N)N=C(OCCCC)N=C2N(CC3=CC=CC(CN4CCCC4)=C3)C1

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 98.80%

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    Product Name:
    Vesatolimod
    Cat. No.:
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    Vesatolimod

    Cat. No.: HY-15601