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CAS No. : 643082-52-4
MCE 国际站:YM-341619
产品活性:YM-341619 (AS1617612) 是一种有效的口服 STAT6 抑制剂,IC50 为 0.70 nM。YM-341619 可抑制 IL-4 诱导的小鼠脾脏 T 细胞 Th2 分化 (IC50=0.28 nM),但不影响 Th1 细胞的分化。YM-341619 是一种很有希望的化合物,可用于过敏性疾病研究的化合物,如过敏性哮喘。
研究领域:JAK/STAT Signaling | Stem Cell/Wnt
作用靶点:STAT
In Vitro: YM-341619 (0.1-100 nM; pretreatment 30 min before IL-4) inhibits IL-4-increased STAT6 luciferase gene activity in a concentration dependent manner, exhibiting an IC50 value of 1.5 nM in FW4 cells.YM-341619 (0.1-10 nM; pretreatment 30 min before IL-4) concentration-dependently decreases the production of IL-4 and the expression of GATA-3 mRNA in T cells cultured with IL-4. And it has no effects on the production of IFN-γ or the expression of T-bet (a Th1 transcription factor) mRNA in T cells cultured with IL-12.
In Vivo: YM-341619 (intravenous injection; 1 mg/kg) exhibits CLtot, t1/2, Vd values of 36.1 mL/min/kg, 1.0 hour, 3117 mL/kg, respectively. And it exhibits Cmax, Tmax, AUC, and F% values of 80 ng/mL, 0.5h, 114 ng h/mL and 25%, respectively in 8-week-old female balb/c mice.YM-341619 (oral administration; 0.003-0.03 mg/kg) suppresses the IgE level in a dose-dependent manner, but not the IgG2a level, and the ED50 value of YM-341619 for the suppression of IgE production is 0.026 mg/kg. YM-341619 tends to decrease IL-4 production and decrease IL-13 production in a dose-dependent manner (both 57%), but does not affect IFN-γ production in DNP-Ascaris-sensitized rats.
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货号: HY-134771
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