Zoniporide (hydrochloride)_钠氢交换同工型1(NHE-1)抑制剂_241800-97-5_Apexbio
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特别声明
产品仅用于研究，
不针对患者销售，望谅解。
每个产品具体的储存和使用信息显示在产品说明书中。ApexBio 产品在推荐的条件下是稳定 的。产品会根据不同的推荐温度进行运输。许多产品短期运输是稳定的，运输温度不同于长 期储存的温度。我们确保我们的产品是在保持试剂质量的条件下运输的。收到产品后，按照 产品说明书上的要求进行储存。
产品说明书化学性质产品名: Zoniporide (hydrochloride) 修订日期: 6/30/2016
产品名: Cas No.: 分子量: 分子式: 别名: 化学名:
SMILES: 溶解性: 储存条件: 一般建议:
运输条件:
Zoniporide (hydrochloride)
241800-97-5 393.3
ApexBio Technology
Store at -20°C For obtaining a higher solubility , please warm the tube at 37°C and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
physiological pH. Hyperactivation of NHE1 during ischemia–reperfusion episodes disrupts the intracellular ion balance, leading to cardiac dysfunction and damage [2]. In vitro: Zoniporide inhibited human NHE-1 with an IC50 of 14 nM, showed >150-fold selectivity against other NHE isoforms, and potently inhibited ex vivo NHE-1-dependent swelling of human platelets. In the isolated heart (Langendorff), zoniporide dose-dependently reduced infarct size with an EC50 of 0.25 nM. Zoniporide at 50 nM reduced infarct size by 83% [1]. In vivo: Zoniporide was well tolerated in preclinical animal models, exhibited moderate plasma protein binding with t1/2 of 1.5 h in monkeys. In rabbit models of myocardial ischemia-reperfusion injury, zoniporide significantly reduced infarct size without adverse effects. In open chest, anesthetized rabbits, zoniporide reduced infarct size in a dose-dependent manner with an ED50 of 0.45 mg/kg/h. Zoniporide also inhibited NHE-1-mediated platelet swelling. Zoniporide attenuated postischemic cardiac contractile dysfunction in conscious primates, and reduced both the incidence and duration of ischemiareperfusion-induced ventricular fibrillation in rats [1].
参考文献: [1] Tracey W R, Allen M C, Frazier D E, et al. Zoniporide: a potent and selective inhibitor of the human sodium-hydrogen exchanger isoform 1 (NHE-1)[J]. Cardiovascular drug reviews, 2003, 21(1): 17-32. [2] Masereel B, Pochet L, Laeckmann D. An overview of inhibitors of Na+/H+ exchanger[J]. European journal of medicinal chemistry, 2003, 38(6): 547-554.
C17H16N6O • HCl
CP 597,396
N-(aminoiminomethyl)-5-cyclopropyl-1-(5-quinolinyl)-1H-pyrazole-4carboxamide, monohydrochloride O=C(C(C=N1)=C(C2CC2)N1C3=C4C(N=CC=C4)=CC=C3)/N=C(N)/N.Cl Soluble in DMSO
生物活性
靶点 :
Membrane Transporter/Ion Channel
信号通路:
sodium-hydrogen exchanger
产品描述:
Zoniporide (hydrochloride) is a novel, potent, and selective sodium-hydrogen exchanger isoform-1 (NHE-1) inhibitor [1]. The Na+/H+ exchanger (NHE) has been involved in intracellular pH homeostasis of many mammalian cell types. Until now, seven NHE isoforms (NHE1–NHE7) have been identified. NHE1 is the most predominant isoform expressed in heart responsible for maintaining cardiomyocyte pH homeostasis. Activation of NHE is essential for the restoration of
产品仅用于研究，
不针对患者销售，望谅解。
每个产品具体的储存和使用信息显示在产品说明书中。ApexBio 产品在推荐的条件下是稳定 的。产品会根据不同的推荐温度进行运输。许多产品短期运输是稳定的，运输温度不同于长 期储存的温度。我们确保我们的产品是在保持试剂质量的条件下运输的。收到产品后，按照 产品说明书上的要求进行储存。
产品说明书化学性质产品名: Zoniporide (hydrochloride) 修订日期: 6/30/2016
产品名: Cas No.: 分子量: 分子式: 别名: 化学名:
SMILES: 溶解性: 储存条件: 一般建议:
运输条件:
Zoniporide (hydrochloride)
241800-97-5 393.3
ApexBio Technology
Store at -20°C For obtaining a higher solubility , please warm the tube at 37°C and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
physiological pH. Hyperactivation of NHE1 during ischemia–reperfusion episodes disrupts the intracellular ion balance, leading to cardiac dysfunction and damage [2]. In vitro: Zoniporide inhibited human NHE-1 with an IC50 of 14 nM, showed >150-fold selectivity against other NHE isoforms, and potently inhibited ex vivo NHE-1-dependent swelling of human platelets. In the isolated heart (Langendorff), zoniporide dose-dependently reduced infarct size with an EC50 of 0.25 nM. Zoniporide at 50 nM reduced infarct size by 83% [1]. In vivo: Zoniporide was well tolerated in preclinical animal models, exhibited moderate plasma protein binding with t1/2 of 1.5 h in monkeys. In rabbit models of myocardial ischemia-reperfusion injury, zoniporide significantly reduced infarct size without adverse effects. In open chest, anesthetized rabbits, zoniporide reduced infarct size in a dose-dependent manner with an ED50 of 0.45 mg/kg/h. Zoniporide also inhibited NHE-1-mediated platelet swelling. Zoniporide attenuated postischemic cardiac contractile dysfunction in conscious primates, and reduced both the incidence and duration of ischemiareperfusion-induced ventricular fibrillation in rats [1].
参考文献: [1] Tracey W R, Allen M C, Frazier D E, et al. Zoniporide: a potent and selective inhibitor of the human sodium-hydrogen exchanger isoform 1 (NHE-1)[J]. Cardiovascular drug reviews, 2003, 21(1): 17-32. [2] Masereel B, Pochet L, Laeckmann D. An overview of inhibitors of Na+/H+ exchanger[J]. European journal of medicinal chemistry, 2003, 38(6): 547-554.
C17H16N6O • HCl
CP 597,396
N-(aminoiminomethyl)-5-cyclopropyl-1-(5-quinolinyl)-1H-pyrazole-4carboxamide, monohydrochloride O=C(C(C=N1)=C(C2CC2)N1C3=C4C(N=CC=C4)=CC=C3)/N=C(N)/N.Cl Soluble in DMSO
生物活性
靶点 :
Membrane Transporter/Ion Channel
信号通路:
sodium-hydrogen exchanger
产品描述:
Zoniporide (hydrochloride) is a novel, potent, and selective sodium-hydrogen exchanger isoform-1 (NHE-1) inhibitor [1]. The Na+/H+ exchanger (NHE) has been involved in intracellular pH homeostasis of many mammalian cell types. Until now, seven NHE isoforms (NHE1–NHE7) have been identified. NHE1 is the most predominant isoform expressed in heart responsible for maintaining cardiomyocyte pH homeostasis. Activation of NHE is essential for the restoration of