| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
SMU-R39 (0.1-30 μM, 24 h) showed strong inhibitory activity against R848-induced SEAP signaling in HEK-Blue hTLR8 cells (IC50 = 0.24 μM) and moderate inhibitory activity against R848-induced SEAP signaling in HEK-Blue hTLR7 cells (IC50 = 3.22 μM) [1]. SMU-R39 (0.01-10 μM, 24 h) significantly blocked the increase in SEAP signaling induced by Resiquimod (R848) in THP1-Dual cells, with an IC50 of 0.18 μM, showing its ability to inhibit NF-κB activation through TLR7/8 signaling [1]. SMU-R39 (0.046-100 μM, 24 h) showed dose-dependent inhibition of R848-activated TLR7/8 activity in HEK-Blue hTLR7/8 and THP1-Dual cells [1]. SMU-R39 (5-10 μM, 0.5 h) downregulated the expression levels of phosphorylated IKKα/β, p65, and p38 proteins in R848-stimulated THP-1 macrophages, and inhibited the downstream NF-κB and MAPK signaling pathways of TLR7/8 [1]. SMU-R39 (0.1-20 μM, 24 h) significantly reduced the secretion of TNF-α in R848-stimulated THP-1 macrophages, Raw 264.7 cells, and PBMCs in a concentration-dependent manner [1]. SMU-R39 (0.1-20 μM, 6 h) effectively reduced the gene expression of TNF-α, IL-1β, IL-8, IL-6, and IFN-β in R848-stimulated THP-1 macrophages and PBMCs [1].
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|---|---|
| ln Vivo |
SMU-R39 (0.5%-1.0% soft, topical, once daily ointment for 7 days) significantly enhances the psoriatic skin barrier in female BALB/c electrodes with Imiquimod (IMQ) induction[1].
|
| Cell Assay |
Real Time qPCR[1]
Cell Types: R848-stimulated THP-1 macrophages and PBMCs Tested Concentrations: 0.1, 1, 10, 20 μM Incubation Duration: 6 h Experimental Results: Decreased the gene expression of TNF-α, IL-1β, IL-8, IL-6, and IFN-β in R848-stimulated THP-1 macrophages and PBMCs[1]. Western Blot Analysis[1] Cell Types: R848-stimulated THP-1 macrophages Tested Concentrations: 5, 10 μM Incubation Duration: 0.5 h Experimental Results: Downregulated the expression levels of phosphorylated IKKα/β, p65, and p38 proteins in R848-stimulated THP-1 macrophages [1]. |
| Animal Protocol |
Animal/Disease Models: IMQ-induced psoriasis mouse model: 5% Imiquimod (IMQ) ointment (62.5 mg) was topically applied to the hairless dorsal skin of 8-12-week-old female BALB/c mice once daily for 7 consecutive days[1]
Doses: 0.5%, 1.0% ointment Route of Administration: topical, once daily, 7 days Experimental Results: Achieved a psoriasis area and severity index (PASI) reduction. Showed no significant changes in body weight. Reduced the Ki67 expression. Downregulated the gene expression of skin TNF-α, IFN-α , IL-17 , IL-22 , and IL-23 . Achieved an epidermal thickness reduction. |
| References |
| Molecular Formula |
C23H25N5O
|
|---|---|
| Molecular Weight |
387.48
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| Appearance |
Typically exists as solids at room temperature
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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)
|
| 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 | 2.5808 mL | 12.9039 mL | 25.8078 mL | |
| 5 mM | 0.5162 mL | 2.5808 mL | 5.1616 mL | |
| 10 mM | 0.2581 mL | 1.2904 mL | 2.5808 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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