909561-15-5
中文名稱
化合物AS1810722
英文名稱
1-Piperazineacetamide, 4-[4-[[7-[(3,5-difluorophenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]-
CAS
909561-15-5
分子式
C25H25F2N7O
分子量
477.51
MOL 文件
909561-15-5.mol
更新日期
2023/03/20 15:41:27
909561-15-5 結(jié)構(gòu)式
基本信息
中文別名
化合物AS1810722 英文別名
AS18107221-Piperazineacetamide, 4-[4-[[7-[(3,5-difluorophenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]-
AS-1810722,inhibit,CYPs,AS 1810722,Cytochrome P450,eosinophil,allergic,AS1810722,STAT,orally,Inhibitor,asthma,IL-4,infiltration,IFN-γ
物理化學(xué)性質(zhì)
沸點(diǎn)731.4±70.0 °C(Predicted)
密度1.41±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO: 62.5 mg/mL (130.89 mM)
酸度系數(shù)(pKa)16.30±0.40(Predicted)
形態(tài)Solid
顏色Brown to black
常見問題列表
生物活性
AS1810722 是口服有效的 STAT6 抑制劑，IC50 為 1.9 nM。AS1810722 顯示出良好的 CYP3A4 抑制作用。AS1810722 具有用于過敏性疾病，例如哮喘和特應(yīng)性疾病研究的潛力。靶點(diǎn)
|
STAT6 1.9 nM (IC 50 ) |
CYP3A4
|
體外研究
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.
體內(nèi)研究
AS1810722 (compound 24) 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.
| Animal Model: | Female Balb/c mice asthmatic model by intraperitoneal injection of 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. |