| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
|
| Targets |
IRF5[1]
|
|---|---|
| ln Vitro |
In human PBMCs and mouse splenocytes, YE6144(1 or 3 μM; 30 min) suppresses the phosphorylation of IRF5[1]. In human HC PBMCs, YE6144(0–10 μM; 30 min) suppresses type I IFN production with an IC50 of roughly 0.09 μM[1].
|
| ln Vivo |
The progression of systemic lupus erythematosus in mice is suppressed by YE6144 (40.0 mg/kg; sc; once)[1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: Human HC PBMCs and mouse WT splenocytes Tested Concentrations: 1 μM(PBMCs) and 3 μM(splenocytes) Incubation Duration: 30 min Experimental Results: Inhibited the phosphorylation of IRF5. RT-PCR[1] Cell Types: Mouse WT splenocytes Tested Concentrations: 3 μM Incubation Duration: 30 min Experimental Results: Induction of type I IFN genes, Ifnb1 and Ifna stimulated by TLR7 ligands or TLR9 ligands was remarkably weakened. |
| Animal Protocol |
Animal/Disease Models: NZB/W F1 mouse model of systemic lupus erythematosus (SLE)[1]
Doses: 40.0 mg/kg Route of Administration: subcutaneous (sc) injection, once Experimental Results: Suppressed the exacerbation of autoantibody production. Splenomegaly and renal dysfunction were also suppressed by the treatment after disease onset. |
| References |
| Molecular Formula |
C21H27CLFN7O
|
|---|---|
| Molecular Weight |
447.94
|
| Appearance |
Orange to red solid powder
|
| 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)
|
| Solubility (In Vitro) |
DMSO :~100 mg/mL (~223.24 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 10 mg/mL (22.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 100.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 10 mg/mL (22.32 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 100.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 10 mg/mL (22.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2324 mL | 11.1622 mL | 22.3244 mL | |
| 5 mM | 0.4465 mL | 2.2324 mL | 4.4649 mL | |
| 10 mM | 0.2232 mL | 1.1162 mL | 2.2324 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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