| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
SMU-L11-R (0-100 μM; 24 h; HEK-Blue hTLR7 cells) showed no significant toxic effects [1]. SMU-L11-R (0-100 μM; 24 h; B16-F10 cells) showed cytotoxic effects at the highest concentration of 100 μM [1]. SMU-L11-R (0, 0.1, 1, 5, 10 μM; 24 h; peritoneal macrophages) showed an increase in M1 macrophages with increasing dose [1][1]. SMU-L11-R (1 μM; 15-120 min; BMDCs) activated downstream signaling pathways of TLR7 via MyD88 protein, including the NF-κB and MAPK signaling pathways [1]. SMU-L11-R (0, 0.01, 0.1, 1, 10 μM; 24 h; HEK-Blue hTLR7 cells) showed a dose-dependent increase in TLR7 protein [1]. SMU-L11-R (0-10 μM; 24 h; Raw 264.7 cells) showed a significant increase in TNF-α and IL-6 [1]. SMU-L11-R (0-10 μM; 24 h; human PBMCs) showed a dose-dependent increase in TNF-α and IL-1β [1]. SMU-L11-R (0-10 μM; 24 h; mouse BMDCs) showed a significant increase in IL-6 [1]. SMU-L11-R (0, 0.1, 1, 10 μM; 24 h; peritoneal macrophages) showed a concentration-dependent increase in NO production [1]. With increasing concentration, SMU-L11-R also showed activation of TLR8 (EC50 = 2.56 μM), but its activation was 156 times lower than that of TLR7. The activation of hTLR2, hTLR3 or hTLR4 induced by SMU-L11-R in HEK-Blue cells was negligible [1].
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|---|---|
| ln Vivo |
SMU-L11-R (5-10 mg/kg; IP; every 2 days; 15 days) inhibits MC38 tumor growth and enhances antitumor effects when conjugated with PD-L1 [1].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: HEK-Blue hTLR7 cells Tested Concentrations: 0.26 μM, 0.52 μM, 1.04 μM, 2.08 μM, 4.17 μM, 8.33 μM, 16.67 μM, 33.33 μM, 100 μM Incubation Duration: 24 h Experimental Results: Showed no obvious toxic effect. Cell Viability Assay[1] Cell Types: MC38 cells Tested Concentrations: 0.02 μM, 0.05 μM, 0.14 μM, 1.23 μM, 11.11 μM, 33.33 μM, 100 μM Incubation Duration: 24 h Experimental Results: Showed cytotoxic effect at a high testing concentration (100 μM). Cell Viability Assay[1] Cell Types: B16-F10 cells Tested Concentrations: 0.26 μM, 0.52 μM, 1.04 μM, 2.08 μM, 4.17 μM, 8.33 μM, 16.67 μM, 33.33 μM, 100 μM Incubation Duration: 24 h Experimental Results: Showed cytotoxic effect at a high testing concentration (100 μM). Western Blot Analysis[1] Cell Types: HEK-Blue hTLR7 cells Tested Concentrations: 0, 0.01, 0.1, 1, 10 μM Incubation Duration: 24 h Experimental Results: Showed dose-dependent increase in TLR7 protein. Western Blot Analysis[1] Cell Types: BMDCs Tested Concentrations: 1 μM Incubation Duration: 15 min, 30 min, 60 min, 90 min, 120 min Experimental Results: Showed significant induction of the phosphorylation of IKK α/ β, p65, p38 and ERK1/2 in BMDCs. ELISA Assay[1] Cell Types: Raw 264.7 cells Tested Concentrations: 0, 0.01, 0.1, 1, 10 μM Incubation Duration: 24 h Experimental Results: Showed significant increase in TNF-α and IL-6. ELISA Assay[1] Cell Types: Mouse BMDCs Tested Concentrations: 0, 0.01, 0.1, 1, 10 μM Incubation Duration: 24 h Experimental Results: Showed significant increase in IL-6. ELISA Assay[1] Cell Types: Human PBMCs Tested Concentrations: 0, 0.01, 0.1, 1, 10 μM Incubation Duration: 24 h Experimental Results: Showed dose-dependent increase in TNF-α and IL-1β. |
| Animal Protocol |
Animal/Disease Models: C57/BL6 wild-type male mice (6-8 weeks old) were injected subcutaneousely with 2 x 105 MC38 cells[1]
Doses: 5 mg/kg, 10 mg/kg Route of Administration: IP; every 2 days; 15 days Experimental Results: Significantly inhibited tumor growth and exhibited excellent synergistic anti-tumor effects when combined with PD-L1 inhibitors by upregulating CD8+ T cells. |
| References |
| Molecular Formula |
C19H24N4O
|
|---|---|
| Molecular Weight |
324.42
|
| CAS # |
3040320-18-8
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| Appearance |
Typically exists as solids at room temperature
|
| 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 | 3.0824 mL | 15.4121 mL | 30.8242 mL | |
| 5 mM | 0.6165 mL | 3.0824 mL | 6.1648 mL | |
| 10 mM | 0.3082 mL | 1.5412 mL | 3.0824 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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