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

GS-9620 (Synonyms: Vesatolimod)

Cat. No.: HY-15601 Purity: 98.78%
Handling Instructions

GS-9620 is a potent and selective orally active agonist of Toll-Like Receptor (TLR)7.

For research use only. We do not sell to patients.
GS-9620 Chemical Structure

GS-9620 Chemical Structure

CAS No. : 1228585-88-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 121 In-stock
5 mg USD 110 In-stock
10 mg USD 180 In-stock
50 mg USD 450 In-stock
100 mg USD 650 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

GS-9620 is a potent and selective orally active agonist of Toll-Like Receptor (TLR)7.

IC50 & Target

TLR7[1]

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

Single oral doses of 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), 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. 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
References
Preparing Stock Solutions
Concentration Volume 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.
Cell Assay
[1]

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]. 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 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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 4.8 mg/mL (Need ultrasonic)

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.78%

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Product Name:
GS-9620
Cat. No.:
HY-15601
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