Zoniporide hydrochloride

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CAS NO:	241800-97-5
包装:	5mg
市场价:	4800元

产品名称

CP-597396 hydrochloride

产品介绍

Zoniporide (CP-597396) hydrochloride 是 1 型钠氢交换剂(NHE-1)的有效和选择性抑制剂。Zoniporide hydrochloride 抑制人 NHE-1 (IC₅₀=14 nM)，与其他 NHE 亚型相比具有大于 150 倍的选择性，并有效抑制离体 NHE-1 依赖性的人血小板溶胀 (IC₅₀=59 nM)。

生物活性

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

IC₅₀& Target

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

体内研究
(In Vivo)

Zoniporide (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_1/2of 1.5 hours in monkeys, and has one major active metabolite^[1].
Zoniporide treatment shows the AUC_0-∞and t_1/2are 0.07 μg h/mL and 0.5 hours, respectively^[2].

Animal Model:	Rabbit^[1]
Dosage:	0.25, 1, 4 mg/kg
Administration:	Every hour for 2 hours; intravenous injection
Result:	Elicited a significant dose-dependent reduction in infarct size in the anesthetized rabbit. The ED₅₀was 0.45 mg/kg/h.

Animal Model:	Rat^[2]
Dosage:	1 mg/kg
Administration:	Intravenous injection(Pharmacokinetic Analysis)
Result:	The AUC_0-∞and t_1/2were 0.07 μg h/mL and 0.5 hours, respectively.

分子量

356.81

Formula

C₁₇H₁₇ClN₆O

CAS 号

241800-97-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.