| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
MyD88-IN-3 (1.1-30 μM) exhibited strong anti-inflammatory effects and significantly inhibited the secretion of IL-6 in mouse macrophages J774A.1 (IC50 = 1.32 μM) and human macrophages THP-1 (IC50 = 0.75 μM) differentiated from PMA[1]. MyD88-IN-3 (10 μM, pretreated for 2 hours, then cotreated with 0.5 μg/mL LPS for 30 minutes) restored the LPS-induced reduction in IκBα expression in J774A.1 macrophages, significantly reduced p38 phosphorylation, inhibited JNK phosphorylation, inhibited p65 phosphorylation and nuclear translocation, and inhibited LPS-induced MAPK pathway activation, leading to c-Jun nuclear translocation in cells[1]. MyD88-IN-3 (5 μM, 10 μM) can inhibit the homodimerization of MyD88 in J774A.1[1]. MyD88-IN-3 (10 μM, 2 h) can inhibit the interaction between MyD88 and TLR4 in J774A.1[1]. MyD88-IN-3 (10 μM, 4 h) can improve the thermal stability of MyD88, and about 50% of MyD88 can be retained at 64 °C[1]. MyD88-IN-3 can effectively bind to the TIR domain (KD = 28.5 μM), but does not show binding affinity to the DD domain (KD = 1.32 M)[1].
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|---|---|
| ln Vivo |
MyD88-IN-3 (500 mg/kg, 1000 mg/kg, by gavage, once daily for 10 days) showed good safety in SD rural mice[1]. MyD88-IN-3 (20 mg/kg, by gavage, over 6 hours) reduced acute lung injury in C57BL/6 sepsis[1]. MyD88-IN-3 (20 mg/kg, by gavage, over 30 minutes) attenuated LPS-induced acute lung injury in C57BL/6 mice[1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: J774A.1 mouse macrophages Tested Concentrations: Pretreatment for 2 h, followed by co-treatment with 0.5 μg/mL LPS for 30 minutes Incubation Duration: 2 h Experimental Results: Restored LPS-induced IκBα degradation and inhibited p38 and JNK phosphorylation. |
| Animal Protocol |
Animal/Disease Models: SD rats[1]
Doses: 500 mg/kg, 1000 mg/kg Route of Administration: Oral gavage, once daily for 10 days Experimental Results: Induced a slight decrease in body weight in the first day, following which body weight progressively returned to levels akin to the control group, with no statistically significant differences noted. Indicated no notable pathological alterations in the organs of mice. Animal/Disease Models: Male C57BL/6 mice, weighing between 18 and 22 g, after the administration of anesthesia, an abdominal incision was performed to reveal the cecum. The cecum was ligated beneath the ileocecal valve with surgical thread and subsequently punctured once with a needle. The abdominal incision was subsequently sutured closed after repositioning[1] Doses: 20 mg/kg Route of Administration: Oral gavage, administer 6 hours before CLP surgery Experimental Results: Markedly diminished the lung wet/dry weight ratio, demonstrating its effectiveness in alleviating sepsis-induced lung edema. Obstructed this cellular influx into BALF, suggesting that MyD88-IN-3 alleviates sepsis-induced pulmonary edema. led to a significant decrease in IL-6. Alleviated lung tissue damage, interstitial edema, pulmonary congestion, inflammatory infiltration, and thickened alveolar septa. Significantly diminished immune cell infiltration, thereby mitigating the inflammatory response. Animal/Disease Models: LPS-Induced Male C57BL/6 mice, weighing between 18 and 22 g Doses: 20 mg/kg Route of Administration: Oral gavage, administer 30 min before LPS. Experimental Results: Markedly diminished the lung wet/dry weight ratio, demonstrating its effectiveness in alleviating sepsis-induced lung edema. Significantly suppressed the increase in total protein concentration and the discharge of immune cells into BALF. Decreased spleen weight and mitigated inflammation. Markedly reduced IL-6 levels in both bronchoalveolar lavage fluid and serum samples. Mitigated augmented alveolar septal thickness, pulmonary congestion, inflammatory infiltration, and lung tissue degradation. Reduced leukocyte infiltration into the alveoli. |
| References |
| Molecular Formula |
C24H24N6O5S
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|---|---|
| Molecular Weight |
508.55
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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)
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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 | 1.9664 mL | 9.8319 mL | 19.6637 mL | |
| 5 mM | 0.3933 mL | 1.9664 mL | 3.9327 mL | |
| 10 mM | 0.1966 mL | 0.9832 mL | 1.9664 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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