AS1810722 is an orally active and potent STAT6 inhibitor with an IC 50 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
In Vitro
AS1810722 (compound 24) inhibits production of IL-4 with an IC 50 of 2.4 nM, but shows no effect on production of IFN-γ. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 . AS1810722 inhibits in vitro Th2 differentiation with an IC 50 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female Balb/c mice asthmatic model by intraperitoneal injection of ovalbumin (OVA)-containing aluminum hydroxide gel Dosage: 0.03-0.3 mg/kg Administration: Orally; 30 min before, and 24 and 48 h after OVA exposure Result: Suppressed eosinophil infiltration in the lung in a dose-dependent manner.
IC50& Target:STAT6 1.9 nM (IC 50 ) CYP3A4
Associated Targets(Human)
STAT6TchemSignal transducer and activator of transcription 6 (1 Activities)
