Art. -Nr.: HY-15601

Vesatolimod

Name: Vesatolimod
Brand: MedChemExpress
SKU: HY-15601
Price: 55.00 USD
Availability: InStock
Rating: 5 (14 reviews)

(Synonyms: GS-9620)

14 Cited Publications

Kundenbewertung

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.

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Reinheit : 99.90%
CAS. Nr.: 1228585-88-3
Formel: C₂₂H₃₀N₆O₂
Molecular Weight:410.51

Speicherung:

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

Vesatolimod Chemical Structure

CAS. Nr.: 1228585-88-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

IC₅₀ & Target

TLR7

Alle Toll-like Receptor (TLR) Isoform-spezifische Produkte anzeigen :

Alle HIV Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	290 nM Compound: 5, GS-9620	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	[PMID: 23961878]
HEK293	EC₅₀	9 μM Compound: 5, GS-9620	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	[PMID: 23961878]

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].

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

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 IFN-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) C_max is 3.6±3.5, 36.8±34.5, and 55.4±81.0 nM, respectively. Peak serum IFN 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].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1228585-88-3
Appearance Solid
Molecular Weight 410.51
Formel C₂₂H₃₀N₆O₂
Color White to yellow
SMILES

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

GS-9620
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (14)

All WBIFHistological Imaging/StainingOthers

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Journal Impact Factor

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
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

Vesatolimod purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2018 Sep 19:9:2022. [Abstract]

The increase in viral production from ACH-2 cells was examined by supernatant p24 antigen levels on day 2.
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

Vesatolimod purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Nov 26;26(23):11441. [Abstract]

Ten-day-old C57BL/6J mice were intraperitoneally inoculated with 10 LD50 of EV-A71-H-MA. One hour after virus infection, the mice were treated with diABZI or GS-9620 （5 mg/kg）once daily for 3 days. Muscle tissues were detected by Western blot assay.
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
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

STING Agonist-Mediated Cytokine Secretion Is Accompanied by Monocyte Apoptosis. [Abstract]

2022 Mar 11;8(3):463-471. PMID: 35132859
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.

Vesatolimod purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2018 May:153:39-48. [Abstract]

GS-9620 (4.5 mg/kg). Paraffin sections of hind limb muscle were incubated with anti-EV71 monoclonal antibody, followed by incubation with mouse anti-rabbit IgG.

Vesatolimod purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2018 May:153:39-48. [Abstract]

Western blot analysis of protein expression showed that EV71 infection upregulated the expression of these proteins, while treatment with GS-9620 (4.5 mg/kg) inhibited their expression.

Vesatolimod purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2018 May:153:39-48. [Abstract]

H&E staining showed more invading neutrophils, and muscle fiber damage was more severe in mice administered inhibitors compared with EV71-infected mice treated with GS-9620 (4.5 mg/kg).
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
Vaccine

A mouse model with age-dependent immune response and immune-tolerance for HBV infection. [Abstract]

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
University of Pennsylvania

2023 Mar, 30523087.
bioRxiv

2019 Nov.

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.67 mg/mL (4.07 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

Vesatolimod

14 Cited Publications

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Vesatolimod

Publications Citing Use of MedChemExpress (MCE) Vesatolimod

Alle Toll-like Receptor (TLR) Isoform-spezifische Produkte anzeigen

Alle HIV Isoform-spezifische Produkte anzeigen