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| 2mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
Purity: =99.20%
| Targets |
G10 targets the STING (stimulator of interferon genes) pathway. STING is a key adaptor protein in the innate immune response to cytosolic DNA. By activating STING, G10 induces the production of type I interferons and other antiviral cytokines. The compound is an indirect activator of STING, meaning it does not bind directly to STING but activates STING-dependent phenotypes through an indirect mechanism. Its human specificity makes it a valuable tool for studying the human STING pathway.
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| ln Vitro |
G10 stimulates transcription in human fibroblasts that is dependent on IFN/IRF3, but not on NF-κB [1]. Human STING-dependent phenotype is indirectly activated by G10 [1]. Independent of IPS-1/MAVS-dependent signaling, G10-mediated IRF3 activation and anti-alphaviral activity take place [1]. Gene expression, G10-mediated IRF3 activation, and anti-alphavirus action all depend on STING [1]. Bioactive interferon production and secretion are induced by G10 in a STING-dependent manner [1]. G10 stimulates the production of innate antiviral mRNA in basic human cells [1].
In vitro, G10 induces STING-dependent synthesis and secretion of bioactive interferon. It induces innate antiviral mRNA expression in primary human cells. The compound has an IC90 of 24.57 μM for inhibiting VEEV replication. It induces transcription of genes dependent on IRF3 and IFN. Its activity is specific to the STING pathway, as it has no effect on NF-κB-dependent transcription. These activities have been characterized in various cell-based models. |
| ln Vivo |
In vivo, G10 has been studied for its antiviral activity against emerging Alphaviruses. By activating STING and inducing interferon production, the compound enhances the innate immune response to viral infections. Its in vivo efficacy in protecting against VEEV and other Alphaviruses has been evaluated in animal models. Specific dosing regimens and detailed efficacy data are available in the scientific literature.
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| Enzyme Assay |
In vitro receptor binding assays for G10 are not typically performed, as it is an indirect activator of STING rather than a direct ligand. Its activity is assessed by measuring STING-dependent downstream signaling events. This includes measuring the induction of IRF3-dependent genes and interferon production. The compound's effects on NF-κB-dependent transcription are assessed to confirm STING specificity. These assays characterize the compound's mechanism of action.
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| Cell Assay |
In vitro cell-based assays for G10 involve treating primary human cells or cell lines with the compound to assess its effects on STING signaling and antiviral activity. Interferon production is measured by ELISA or bioassay. Antiviral activity is assessed by measuring the replication of VEEV or other Alphaviruses in infected cells. Gene expression is measured by qPCR. These assays characterize the compound's antiviral and immunostimulatory activities.
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| Animal Protocol |
In vivo animal experiments for G10 have been conducted in models of Alphavirus infection. Animals are infected with VEEV or other Alphaviruses and treated with G10. Efficacy endpoints include survival rates, viral load reduction, and clinical signs of infection. The compound's ability to induce interferon production in vivo is also assessed. These studies support its potential as an antiviral agent.
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| ADME/Pharmacokinetics |
G10 has a molecular weight of 430.88 and a molecular formula of C21H16ClFN2O3S. It is a human-specific STING agonist. The compound is typically dissolved in DMSO for in vitro studies and formulated for in vivo administration. It has a purity of ≥98%. It is typically stored at -20°C. Its chemical name is 4-(2-Chloro-6-fluorobenzyl)-N-(furan-2-ylmethyl)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide.
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| Toxicity/Toxicokinetics |
Specific toxicity data for G10 is not extensively reported. As a STING agonist, its safety profile is related to its effects on the innate immune system. The compound induces interferon production, which may have adverse effects at high doses. Comprehensive toxicological studies would be required for therapeutic development. Standard safety precautions should be taken when handling the compound.
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| References | |
| Additional Infomation |
G10 is a novel human-specific STING agonist that induces interferon production and has antiviral activity against Alphaviruses. It is an indirect activator of STING signaling. The compound has an IC90 of 24.57 μM against VEEV. G10 is a valuable tool for studying the human STING pathway and has potential therapeutic applications in antiviral research.
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| Molecular Formula |
C21H16CLFN2O3S
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|---|---|
| Molecular Weight |
430.87
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| Exact Mass |
430.055
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| CAS # |
702662-50-8
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| Related CAS # |
702662-50-8
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| PubChem CID |
5077622
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
668.3±55.0 °C at 760 mmHg
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| Flash Point |
358.0±31.5 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.651
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| LogP |
3.41
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
613
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NAGKYJATVFXZKN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H16ClFN2O3S/c22-16-4-1-5-17(23)15(16)11-25-18-9-13(6-7-19(18)29-12-20(25)26)21(27)24-10-14-3-2-8-28-14/h1-9H,10-12H2,(H,24,27)
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| Chemical Name |
4-(2-Chloro-6-fluorobenzyl)-N-(furan-2-ylmethyl)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide
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| Synonyms |
G10 G-10 G 10 STING agonist G10
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~75 mg/mL (~174.06 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.80 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3209 mL | 11.6044 mL | 23.2089 mL | |
| 5 mM | 0.4642 mL | 2.3209 mL | 4.6418 mL | |
| 10 mM | 0.2321 mL | 1.1604 mL | 2.3209 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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