Physicochemical Properties
| Molecular Formula | C18H14F3N3O5S2 |
| Molecular Weight | 473.45 |
| Appearance | Typically exists as solid at room temperature |
| 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 | STING-IN-8 (0.1, 0.3, 1, 3 μM, 5 h) inhibits the up-regulation of p-TBK1 and p-IRF3 induced by MSA-2 (10 μM) or 2', 3'-cGAMP (10 μM) in human and mouse cells[1]. STING-IN-8 shows negligible cytotoxicity at a CC50 of 30 μM in THP1-Dual and RAW-Lucia cell lines[1]. STING-IN-8 (0.3, 1, 3 μM and 0.1, 1, 3 μM, 9 h) effectively inhibits STING downstream immune inflammatory cytokines in human and mouse immune cells[1]. |
| ln Vivo | Pharmacokinetic parameters of STING-IN-8 in mice[1] |
| Cell Assay |
Western Blot Analysis[1] Cell Types: Human monocyte derived THP1-Dual cell line, murine macrophage cells and mouse embryonic fibroblasts Concentration: 0.1, 0.3, 1, 3 μM Incubation Duration: 5 h Experimental Results: Significantly down-regulate the the levels of phosphorylated TBK1 and IRF3 induced by MSA-2 (10 μM) and 2’, 3’ -cGAMP (10 μM) in all cell lines with better potency than SN-011 (HY-145010). Real Time qPCR[1] Cell Types: THP1-Dual cell line and RAW-Lucia Tested Concentrations: 0.3, 1, 3 μM and 0.1, 1, 3 μM Incubation Duration: 9 h Experimental Results: Significantly inhibited the MSA-2 (10 μM) or 2’, 3’-cGAMP (10 μM)-induced upregulation of STING signals expression in THP1-Dual cell line and RAW-Lucia cells. |
| Animal Protocol |
Animal/Disease Models:C57BL/6 mice Doses: 10 MG/KG Route of Administration: i.p., a single dose Experimental Results: Effectively reduced MSA-2 (10 MG/KG) -stimulated serum IL-6, CXCL10 levels and inhibited the expression of IFNβ, TNFα, ISG15, ISG56, Cxcl10, IL6 in kidney tissues[1] |
| References |
[1]. Design, synthesis, and evaluation of thiazolecarboxamide derivatives as stimulator of interferon gene inhibitors[J]. Mol Divers. 2024 Apr 29, 1573-501X |
Solubility Data
| Solubility (In Vitro) | May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples |
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1122 mL | 10.5608 mL | 21.1216 mL | |
| 5 mM | 0.4224 mL | 2.1122 mL | 4.2243 mL | |
| 10 mM | 0.2112 mL | 1.0561 mL | 2.1122 mL |