AS1810722是口服有效的STAT6抑制剂，IC50为1.9nM。AS1810722显示出良好的CYP3A4抑制作用。AS1810722是一种稠合双环嘧啶衍生物，具有用于过敏性疾病，例如哮喘和特应性疾病研究的潜力。
货号:ajcx32034
CAS:909561-15-5
分子式:C25H25F2N7O
分子量：477.51
溶解度:DMSO: 62.5 mg/mL (130.89 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

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: Female Balb/c mice asthmatic model by intraperitoneal injection of ovalbumin (OVA)-containing aluminum hydroxide gel[1]

[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.