Zoniporide hydrochloride hydrate  (Synonyms: CP-597396 hydrochloride hydrate)

Zoniporide (CP-597396) hydrochloride hydrate is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride hydrate inhibits human NHE-1 (IC₅₀=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride hydrate potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC₅₀=59 nM)^[1][2].

IC50: 14 nM (NHE-1)^[1]

Zoniporide hydrochloride hydrate (0.25-4 mg/kg; i.v.; every hour for 2 hours) elicits a dose-dependent reduction in infarct size (ED₅₀=0.45 mg/kg/h) in open chest anesthetized rabbits^[1].
Zoniporide exhibits moderate plasma protein binding, has a t_1/2 of 1.5 hours in monkeys, and has one major active metabolite^[1].
Zoniporide hydrochloride hydrate treatment shows the AUC_0-∞ and t_1/2 are 0.07 μg h/mL and 0.5 hours, respectively^[2].

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

374.82

C₁₇H₁₉ClN₆O₂

863406-85-3

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

• [1]. Tracey WR, et al. Zoniporide: a potent and selective inhibitor of the human sodium-hydrogen exchanger isoform 1 (NHE-1). Cardiovasc Drug Rev. 2003 Spring;21(1):17-32.  [Content Brief]

  [2]. Guzman-Perez A, et al. Discovery of zoniporide: a potent and selective sodium-hydrogen exchanger type 1 (NHE-1) inhibitor with high aqueous solubility. Bioorg Med Chem Lett. 2001 Mar 26;11(6):803-7.  [Content Brief]