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| Bioactivity |
AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research[1]. |
| Invitro |
AS1810722 (compound 24) inhibits production of IL-4 with an IC50 of 2.4 nM, but shows no effect on production of IFN-γ[1]. |
| In Vivo |
AS1810722 (compound 24; 0.03-0.3 mg/kg; orally; 30 min before, and 24h and 48 h after OVA exposure) suppress eosinophil infiltration in the lung in a dose-dependent manner in an antigen-induced mouse asthmatic model[1]. AS1810722 inhibits in vitro Th2 differentiation with an IC50 of 2.4 nM without affecting type 1 helper T (Th1) cell differentiation and eosinophil infiltration in an antigen-induced mouse asthmatic model after oral administration[1]. Animal Model: |
| Name |
AS1810722 |
| CAS |
909561-15-5 |
| Formula |
C25H25F2N7O |
| Molar Mass |
477.51 |
| Appearance |
Solid |
| Transport |
Room temperature in continental US; may vary elsewhere. |
| Storage |
| Powder |
-20°C |
3 years |
|
4°C |
2 years |
| In solvent |
-80°C |
6 months |
|
-20°C |
1 month |
|
| Reference |
[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. |
