STING agonist-1 (G10) is a human-specific STING agonist that elicits anti-viral effect against emerging alphaviruses. G10 can effectively inhibit the replication of alphavirus VEEV, with an IC90 value of 24.57 μM.

Physicochemical Properties

Molecular Formula	C21H16CLFN2O3S
Molecular Weight	430.87
Exact Mass	430.055
CAS #	702662-50-8
Related CAS #	702662-50-8
PubChem CID	5077622
Appearance	White to off-white solid powder
Density	1.4±0.1 g/cm3
Boiling Point	668.3±55.0 °C at 760 mmHg
Flash Point	358.0±31.5 °C
Vapour Pressure	0.0±2.0 mmHg at 25°C
Index of Refraction	1.651
LogP	3.41
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	5
Heavy Atom Count	29
Complexity	613
Defined Atom Stereocenter Count	0
InChi Key	NAGKYJATVFXZKN-UHFFFAOYSA-N
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)
Chemical Name	4-(2-Chloro-6-fluorobenzyl)-N-(furan-2-ylmethyl)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide
Synonyms	G10 G-10 G 10 STING agonist G10
HS Tariff Code	2934.99.9001
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)

Biological Activity

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].

References

[1]. Characterization of a Novel Human-Specific STING Agonist that Elicits Antiviral Activity Against Emerging Alphaviruses. PLoS Pathog. 2015 Dec 8;11(12):e1005324.

Solubility Data

Solubility (In Vitro)

DMSO : ~75 mg/mL (~174.06 mM)

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.