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. YM-341619 is a promising compound for the the research of allergic diseases, such as allergic asthma.

Solid

STAT6 0.70 nM (IC50)

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.
has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Shinya Nagashima, et al. Identification of 4-benzylamino-2-[(4-morpholin-4-ylphenyl)amino]pyrimidine-5-carboxamide derivatives as potent and orally bioavailable STAT6 inhibitors. Bioorg Med Chem. 2008 Jul 1;16(13):6509-21. 9.15
[2]. Keiko Ohga,et al.YM-341619 suppresses the differentiation of spleen T cells into Th2 cells in vitro, eosinophilia, and airway hyperresponsiveness in rat allergic models. Eur J Pharmacol. 2008 Aug 20;590(1-3):409-16.

In Vitro: DMSO : 50 mg/mL (109.07 mM; ultrasonic and warming and heat to 60°C)配制储备液