| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
AS2677131 inhibited the production of IL-12p40 with an IC50 value of 2.4 nM and reduced the levels of IL-1β and IL-6 in RAW264.7 mouse macrophages [1]. AS2677131 (0.1-10000 nM) inhibited IL-12p40 and IL-6 in mouse peritoneal macrophages [1]. AS2677131 (0.1-10000 nM) inhibited IL-12p40 and IL-6 in mouse bone marrow-derived dendritic cells [1]. AS2677131 (10 μM) had no significant effect on intracellular Ca2+ influx in Ramos cells [1]. AS2677131 (200 nM) inhibited the production of PI (3,5) P2 in RAW264.7 cells with an inhibition rate of over 90% [1]. AS2677131 (100 nM, 2 h) increased the volume of RAW264.7 cells and induced the production of numerous small vesicles in the cytoplasm [1]. AS2677131 (10-100 nM, 2 h) decreased the activity of promoters in RAW264.7 cells and inhibited the binding of c-Rel to the promoters of IL-12p40 and IL-1β [1]. AS2677131 (100 nM, 2 h) decreased the level of p-Akt in RAW264.7 cells [1].
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|---|---|
| ln Vivo |
AS2677131 (1–30 mg/kg, pathway) reduced the levels of IL-12p40, IL-6, and TNFα in Poly (I:C) and MDP-treated polymers[1]. AS2677131 (1–10 mg/kg, pathway) reduced the expression of MHC class II molecules on the surface of CD45R+ B cells[1]. AS2677131 (1–10 mg/kg, wall, once daily for 24 days) attenuated the trigger for adjuvant-induced arthritis[1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: RAW264.7 cells Tested Concentrations: 100 nM Incubation Duration: 2 h Experimental Results: Reduced p-Akt levels. |
| Animal Protocol |
Animal/Disease Models: Rats with adjuvant-induced arthritis[1]
Doses: 1, 3 and 10 mg/kg Route of Administration: Orally administration, daily for 24 days Experimental Results: Reduced paw swelling (swelling inhibition rates of 34.3% and 78.3% at doses of 3 and 10 mg/kg, respectively). Reversed body weight loss. Decreased joint histological scores (including bone destruction, cartilage destruction, synovial thickening, and inflammatory cell infiltration. Reduced the proportion of CD3-CD45RA+CD62Llow activated B cells in peripheral blood. |
| References |
| Molecular Formula |
C27H30N6O2
|
|---|---|
| Molecular Weight |
470.57
|
| CAS # |
2171502-44-4
|
| Appearance |
Typically exists as solids at room temperature
|
| 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) |
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
|
|---|---|
| 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 | 2.1251 mL | 10.6254 mL | 21.2508 mL | |
| 5 mM | 0.4250 mL | 2.1251 mL | 4.2502 mL | |
| 10 mM | 0.2125 mL | 1.0625 mL | 2.1251 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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