GNE-9822 is a potent, orally active and selective ITK inhibitor with a K i value of 0.7 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma.
性状
Solid
体外研究(In Vitro)
GNE-9822 (compound 28) 抑制 PLCγ 的磷酸化,IC50 值为 55 nM。 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
GNE-9822 (compound 28; po and iv; 1 and 5 mg/kg) 在小鼠和大鼠中观察到良好的生物利用度和半衰期。 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: BALB/c mouse and Sprague-Dawley rats
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Burch JD, et, al. Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors. J Med Chem. 2014 Jul 10;57(13):5714-27.
溶解度数据
In Vitro: DMSO : 62.5 mg/mL (148.61 mM; Need ultrasonic)配制储备液