Zoniporide hydrochloride hydrate|863406-85-3|-陌孚医药/Medlife

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Zoniporide hydrochloride hydrate

目录号: PL07613 纯度: ≥99.0%

CAS No. :863406-85-3

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中文名称	Zoniporide hydrochloride hydrate
中文别名	5-cyclopropyl-N-(diaminomethylidene)-1-quinolin-5-ylpyrazole-4-carboxamide,hydrate,hydrochloride
英文名称	Zoniporide hydrochloride hydrate
英文别名	Zoniporide hydrochloride monohydrate;Zoniporide hydrochloride hydrate;Zoniporide (hydrochloride hydrate);70297XU9ZO;Zoniporide monohydrochloride monohydrate;[1-(Quinolin-5-yl)-5-cyclopropyl-1H-pyrazole-4-carbonyl]guanidine hydrochloride monohydrate;1H-Pyrazole-4-carboxamide, N-(aminoiminomethyl)-5-cyclopropyl-1-(5-quinolinyl)-, hydrochloride, hydrate (1:1:1);Zoniporide hy
Cas No.	863406-85-3
分子式	C₁₇H₁₉ClN₆O₂
分子量	374.82
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	Zoniporide (CP-597396) hydrochloride hydrate 是 1 型钠氢交换剂 (NHE-1) 的有效和选择性抑制剂。Zoniporide hydrochloride hydrate 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 hydrate is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride hydrate inhibits human NHE-1 (IC 50 =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 (IC 50 =59 nM).
性状	Solid
IC50 & Target[1][2]	IC50: 14 nM (NHE-1)
体内研究(In Vivo)	Zoniporide hydrochloride hydrate (0.25-4 mg/kg; i.v.; every hour for 2 hours) elicits a dose-dependent reduction in infarct size (ED 50 =0.45 mg/kg/h) in open chest anesthetized rabbits. Zoniporide exhibits moderate plasma protein binding, has a t 1/2 of 1.5 hours in monkeys, and has one major active metabolite. Zoniporide hydrochloride hydrate treatment shows the AUC 0-∞ and t 1/2 are 0.07 μg h/mL and 0.5 hours, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[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. [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.

溶解度数据	In Vitro: H₂O : 2 mg/mL (5.34 mM; Need ultrasonic and warming)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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