| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
STAT6 1.9 nM (IC50) CYP3A4
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|---|---|
| ln Vitro |
AS1810722 (compound 24) has no effect on the production of IFN-γ but suppresses the synthesis of IL-4 with an IC50 of 2.4 nM [1].
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| ln Vivo |
In an antigen-induced mouse asthma paradigm called Infiltration, AS1810722 (Compound 24; 0.03-0.3 mg/kg; oral; 30 minutes before OVA exposure, 24 hours, and 48 hours after OVA exposure) suppresses pulmonary eosinophils in a dose-dependent manner[1]. In an antigen-induced mouse asthma model, AS1810722 suppresses Th2 differentiation in vitro with an IC50 of 2.4 nM following oral administration; it has no effect on the differentiation of type 1 helper T (Th1) cells or eosinophil infiltration[1].
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| Animal Protocol |
Animal/Disease Models: Female balb/c (Bagg ALBino) mouse asthmatic model by intraperitoneal (ip) injection of ovalbumin (OVA)-containing aluminum hydroxide gel[1]
Doses: 0.03-0.3 mg/kg Route of Administration: po (oral gavage) 30 min before, and 24 and 48 h after OVA exposure Experimental Results: Suppressed eosinophil infiltration in the lung in a dose-dependent manner. |
| References |
[1]. Shinya Nagashima, et al. Novel 7H-pyrrolo[2,3-d]pyrimidine derivatives as potent and orally active STAT6 inhibitors. Bioorg Med Chem. 2009 Oct 1;17(19):6926-36.
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| Molecular Formula |
C25H25F2N7O
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|---|---|
| Molecular Weight |
477.51
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| CAS # |
909561-15-5
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| SMILES |
FC1C=C(C=C(C=1)CN1C=CC2=CN=C(N=C12)NC1C=CC(=CC=1)N1CCN(CC(N)=O)CC1)F
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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) |
DMSO: 62.5 mg/mL (130.89 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.36 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0942 mL | 10.4710 mL | 20.9420 mL | |
| 5 mM | 0.4188 mL | 2.0942 mL | 4.1884 mL | |
| 10 mM | 0.2094 mL | 1.0471 mL | 2.0942 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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