Zoniporide (hydrochloride)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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 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].
References:
[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.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 393.3 |
Cas No. | 241800-97-5 |
Formula | C17H16N6O·HCl |
Synonyms | CP 597,396 |
Solubility | ≤1mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide |
Chemical Name | N-(aminoiminomethyl)-5-cyclopropyl-1-(5-quinolinyl)-1H-pyrazole-4-carboxamide, monohydrochloride |
SDF | Download SDF |
Canonical SMILES | O=C(C(C=N1)=C(C2CC2)N1C3=C4C(N=CC=C4)=CC=C3)/N=C(N)/N.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |