Vesatolimod
Based on 14 publication(s) in Google Scholar
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.
- Purity: 99.90%
- CAS No.: 1228585-88-3
- Formula: C22H30N6O2
- Molecular Weight:410.51
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Vesatolimod
More- Nat Biomed Eng. 2018 Aug;2(8):578-588. [Abstract]
- Hepatology. 2025 Nov 7. [Abstract]
- PLoS Pathog. 2025 Dec 9;21(12):e1013709. [Abstract]
- Int J Mol Sci. 2025 Nov 26;26(23):11441. [Abstract]
- Front Microbiol. 2018 Sep 19:9:2022. [Abstract]
- Antiviral Res. 2022 Sep:205:105384. [Abstract]
- Antiviral Res. 2018 May:153:39-48. [Abstract]
- J Pharm Sci. 2025 Oct 9;115(1):104019. [Abstract]
- ACS Infect Dis. 2023 Jan 13;9(1):23-32. [Abstract]
- ACS Infect Dis. 2022 Mar 11;8(3):463-471. [Abstract]
- Vaccine. 2018 Feb 1;36(6):794-801. [Abstract]
- Drug Test Anal. 2019 Feb;11(2):240-249. [Abstract]
- University of Pennsylvania. 2023 Mar, 30523087.
- bioRxiv. 2019 Nov.
Customer Validation & Images
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WB
Biological Activity
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TLR7 |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | EC50 |
290 nM
Compound: 5, GS-9620
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Agonist activity at human TLR7 expressed in HEK293 cells by reporter based assay
Agonist activity at human TLR7 expressed in HEK293 cells by reporter based assay
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[PMID: 23961878] |
| HEK293 | EC50 |
9 μM
Compound: 5, GS-9620
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Agonist activity at human TLR8 expressed in HEK293 cells by reporter based assay
Agonist activity at human TLR8 expressed in HEK293 cells by reporter based assay
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[PMID: 23961878] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1228585-88-3
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Appearance Solid
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Molecular Weight 410.51
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Formula C22H30N6O2
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Color White to yellow
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SMILES
O=C1NC2=C(N)N=C(OCCCC)N=C2N(CC3=CC=CC(CN4CCCC4)=C3)C1
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Synonyms
GS-9620
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (14)
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Journal Impact Factor
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Most Recent
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Nat Biomed Eng
TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]2018 Aug;2(8):578-588. PMID: 31015631 -
Hepatology
GPC3-based circular RNA vaccine suppresses hepatocellular carcinoma progression by activating adaptive immune responses. [Abstract]2025 Nov 7. PMID: 41201153 -
PLoS Pathog
Antiviral and immune modulatory activities of STING agonists in a mouse model of persistent hepatitis B virus infection. [Abstract]2025 Dec 9;21(12):e1013709. PMID: 41364734 -
Int J Mol Sci
STING Restricts EV-A71 Infection by Regulating T Cell Development and Enhancing Immune Cell Effector Function. [Abstract]2025 Nov 26;26(23):11441. PMID: 41373601 -
Front Microbiol
Combination of a Latency-Reversing Agent With a Smac Mimetic Minimizes Secondary HIV-1 Infection in vitro. [Abstract]2018 Sep 19:9:2022. PMID: 30283406 -
Antiviral Res
Antiviral effect of vesatolimod (GS-9620) against foot-and-mouth disease virus both in vitro and invivo. [Abstract]2022 Sep:205:105384. PMID: 35863499 -
Antiviral Res
GS-9620 inhibits enterovirus 71 replication mainly through the NF-κB and PI3K-AKT signaling pathways. [Abstract]2018 May:153:39-48. PMID: 29425831
Vesatolimod purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2018 May:153:39-48. [Abstract]
The expression of proteins is determined by western blot, which are up-regulated by EV71 infection and repressed by GS-9620 treatment.
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J Pharm Sci
Investigation of synergistic effects of β-defensin, vesatolimod and resiquimod in increasing the potency of a therapeutic HIV-1 vaccine candidate. [Abstract]2025 Oct 9;115(1):104019. PMID: 41067501 -
ACS Infect Dis
Synthetic Stimulator of Interferon Genes (STING) Agonists Induce a Cytokine-Mediated Anti-Hepatitis B Virus Response in Nonparenchymal Liver Cells. [Abstract]2023 Jan 13;9(1):23-32. PMID: 36472628 -
ACS Infect Dis
2022 Mar 11;8(3):463-471. PMID: 35132859 -
Vaccine
2018 Feb 1;36(6):794-801. PMID: 29306503 -
Drug Test Anal
Metabolism of vesatolimod in rat, dog, and human liver microsomes: Metabolic stability assessment, metabolite identification, and interspecies comparison. [Abstract]2019 Feb;11(2):240-249. PMID: 30129284 -
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Solvent & Solubility
DMSO : ≥ 16.67 mg/mL (40.61 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (4.07 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1.67 mg/mL (4.07 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Rebbapragada I, et al. Molecular Determinants of GS-9620-Dependent TLR7 Activation. PLoS One. 2016 Jan 19;11(1):e0146835. [Content Brief]
[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. [Content Brief]
[3]. D Tumas, et al. Preclinical Characterization of GS-9620, A Potent and Selective Oral TLR7 Agonist.
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4360 mL | 12.1800 mL | 24.3599 mL | 60.8999 mL |
| 5 mM | 0.4872 mL | 2.4360 mL | 4.8720 mL | 12.1800 mL | |
| 10 mM | 0.2436 mL | 1.2180 mL | 2.4360 mL | 6.0900 mL | |
| 15 mM | 0.1624 mL | 0.8120 mL | 1.6240 mL | 4.0600 mL | |
| 20 mM | 0.1218 mL | 0.6090 mL | 1.2180 mL | 3.0450 mL | |
| 25 mM | 0.0974 mL | 0.4872 mL | 0.9744 mL | 2.4360 mL | |
| 30 mM | 0.0812 mL | 0.4060 mL | 0.8120 mL | 2.0300 mL | |
| 40 mM | 0.0609 mL | 0.3045 mL | 0.6090 mL | 1.5225 mL |
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