Zoniporide hydrochloride 是一种特异性的 NHE-1 抑制剂,IC50 为 14 nM,是其他 NHE 同工型的 >150 倍特异性。 Zoniporide hydrochloride 对人血小板的 NHE-1 依赖性肿胀的 IC50 为 59 nM。
产品描述
Zoniporide hydrochloride is a selective inhibitor of NHE-1 with IC50 of 14 nM which is >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride shows an IC50 of 59 nM for NHE-1-dependent swelling of human platelets.
体内活性
In rats, Zoniporide hydrochloride (1 mg/kg; i.v.) shows the AUC0-∞ and t1/2 are 0.07 μg h/mL and 0.5 hours, respectively[1]. In open chest anesthetized rabbits, Zoniporide hydrochloride (0.25, 1, 4 mg/kg; i.v.) dose-dependently reduces infarct size with an ED50 of 0.45 mg/kg/h. Zoniporide hydrochloride exhibits moderate plasma protein binding with t1/2 of 1.5h in monkeys[2].
Cas No.
241800-97-5
分子式
C17H17ClN6O
分子量
356.81
别名
CP-597396 hydrochloride
储存和溶解度
DMSO:Soluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years