KCC2 blocker 1 is an orally active and selective K-Cl cotransporter KCC2 blocker with an IC 50 of 1 μM. KCC2 blocker 1 is a benzyl prolinate.
性状
Solid
IC50 & Target[1][2]
IC50: 1 μM (KCC2)
体外研究(In Vitro)
KCC2 blocker 1 (compound 13; 100 μM) inhibits NKCC1 with 35%. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
KCC2 blocker 1 (compound 13; 1 mg/kg iv and 6 mg/kg po) has a t 1/2 of 0.3 hours, a CL of 26 mL/min/kg, a C max of 457 ng/mL and a AUC of 726 ng?h/mL for male Wistar rats. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
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]. Pégurier C, et al. Benzyl prolinate derivatives as novel selective KCC2 blockers. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2542-5.
溶解度数据
In Vitro: DMSO : 250 mg/mL (601.68 mM; Need ultrasonic)配制储备液