| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Sim-9 (2.5–10 μM) dose-dependently inhibited the interferon response induced by TLR/RLR/STING activation in mouse RAW264.7 cells and human THP-1/HT-29/A549 cells [1]. Sim-9 (5 μM; 0.5–6 h) inhibited IRF3 phosphorylation activated by the cGAS-STING, TLR3, or RIG-I pathways in mouse RAW264.7 cells without affecting TBK1 phosphorylation [1]. Sim-9 (5 μM) inhibited IRF3 homodimerization activated by the cGAS-STING, TLR3, or RIG-I pathways in mouse RAW264.7 cells [1].
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|---|---|
| ln Vivo |
Sim-9 (30-60 mg/kg; intraperitoneal injection; single injection) has shown protective and anti-inflammatory activity in a mouse sepsis model [1]. Sim-9 (30-60 mg/kg; intraperitoneal injection; single injection/triple injection) improved pancreatic edema and inflammatory marker levels in a mouse model of acute pancreatitis [1].
|
| Cell Assay |
Western Blot Analysis [1]
Cell Types: Mouse RAW264.7 cells Tested Concentrations: 5 μM Incubation Duration: 0.5, 1, 2, 4, 6 hours Experimental Results: Phosphorylated IRF3 levels decreased significantly starting 1 hour after stimulation, with the inhibitory effect lasting up to 6 hours. It had no effect on phosphorylated or total TBK1 protein levels. |
| Animal Protocol |
Animal/Disease Models:C57BL/6J mice (8-week-old males, weighing 0.022-0.024 kg, sepsis induced by cecal ligation and puncture) [1]
Doses: 30 mg/kg; 60 mg/kg Route of Administration: Intraperitoneal injection; single injection 2 hours before surgery Experimental Results: The mortality rate of sepsis induced by cecal ligation and puncture was reduced to 60% and 80%, respectively. Survival rate was significantly improved. Systemic inflammatory response was inhibited and IRF3-mediated inflammatory damage in the kidney and lung tissues was reduced. Animal/Disease Models:C57BL/6J mice (8-week-old males, 0.022–0.024 kg, acute pancreatitis induced by secretin) [1] Doses: 30 mg/kg; 60 mg/kg Route of Administration: Intraperitoneal injection; 1 hour before the first injection of secretin (acute phase); 3 injections in total: 1 hour before the first injection of secretin, 24 hours after the first injection of secretin, and 48 hours after the first injection of secretin (recovery phase) Experimental Results: Both doses significantly reduced pancreatic edema, pancreatic weight, and serum amylase and lipase levels during the acute phase. Both doses improved pancreatic histology during the acute phase (reducing acinar cell edema, necrosis, and immune cell infiltration). Both doses significantly reduced serum amylase and lipase levels during the recovery phase. Both doses improved pancreatic histology during the recovery period (reducing acinar cell necrosis and acinar-ductal metaplasia). Both doses reduced p-IRF3 staining in pancreatic tissue during the recovery period. Both doses reduced CD11b-IRF7 colocalization in pancreatic tissue during the recovery period. |
| References |
| Molecular Formula |
C31H28F3NO6
|
|---|---|
| Molecular Weight |
567.55
|
| CAS # |
3099101-40-0
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| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(C1=CC=C(C2=CC=C(C=C2)C(F)(F)F)O1)OC3=C4[C@]56[C@@](C=C(C(C6)=O)OC)([H])[C@](N(CC5)C)([H])CC4=CC=C3OC
|
| 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) |
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
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|---|---|
| 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7620 mL | 8.8098 mL | 17.6196 mL | |
| 5 mM | 0.3524 mL | 1.7620 mL | 3.5239 mL | |
| 10 mM | 0.1762 mL | 0.8810 mL | 1.7620 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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