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。

YM-341619 (AS1617612) is a potent and orally active STAT6 inhibitor with an IC 50 of 0.70 nM. YM-341619 inhibits Th2 differentiation in mouse spleen T cells induced by IL-4 ( IC 50 =0.28 nM) without affecting Th1 cell differentiation [1]. YM-341619 is a promising compound for the the research of allergic diseases, such as allergic asthma [2].

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 IC 50 value of 1.5 nM in FW4 cells [2].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 [2]. RT-PCR [2] Cell Line: T cells Concentration: 0.1 nM, 1 nM, 10 nM Incubation Time: Pretreatment 30 min before IL-4, then IL-4 treated for 16 hours Result: Decreased IL-4 and GATA-3 mRNA expression.

YM-341619 (intravenous injection; 1 mg/kg) exhibits CL tot, t 1/2, V d values of 36.1 mL/min/kg, 1.0 hour, 3117 mL/kg, respectively. And it exhibits C max, T max, 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 [1].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 ED 50 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 [2]. Animal Model: DNP-Ascaris-sensitized rats [1] Dosage: 0.003-0.03 mg/kg Administration: Oral administration; 0.003-0.03 mg/kg Result: Suppressed IL-4 and IL-13 production in splenocytes derived from DNP-ascaris-sensitized rats without reducing IFN-γ production.

643082-52-4

C22H21F3N6O2

458.44

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years