249296-45-5
Chemical Structure
Zoniporide mesylate
Synonym(s): CP-597396 mesylate
- CAS. Nr.: 249296-45-5
- Formula:C18H20N6O4S
- Molecular Weight:416.45
IUPAC Name: N-carbamimidoyl-5-cyclopropyl-1-(quinolin-5-yl)-1H-pyrazole-4-carboxamide methanesulfonate
InChIKey: LEHNUSLKIYRRQJ-UHFFFAOYSA-N
SMILES: N=C(N)NC(C1=C(C2CC2)N(C3=C4C(N=CC=C4)=CC=C3)N=C1)=O.CS(=O)(O)=O
Biological Activity: Zoniporide mesylate (CP-597396 mesylate) is a selective Na+/H+ exchanger subtype 1 (NHE1) inhibitor with cardioprotective activity, with IC50 values of 67 nM and 73 nM against rat NHE1. Zoniporide mesylate reduces intracellular Na+ and Ca2+ overload, preserves mitochondrial integrity, activates pro-survival ERK1/2 and STAT3 signaling pathways, reduces necrosis and apoptosis, and decreases neutrophil aggregation. Zoniporide mesylate is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury[1][2][3][4][5].
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Zoniporide mesylate | Zoniporide mesylate (CP-597396 mesylate) is a selective Na+/H+ exchanger subtype 1 (NHE1) inhibitor with cardioprotective activity, with IC50 values of 67 nM and 73 nM against rat NHE1. Zoniporide mesylate reduces intracellular Na+ and Ca2+ overload, preserves mitochondrial integrity, activates pro-survival ERK1/2 and STAT3 signaling pathways, reduces necrosis and apoptosis, and decreases neutrophil aggregation. Zoniporide mesylate is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury. | |||||||||||||||||||||
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- [1]. Gao L, et al. Critical role of the STAT3 pathway in the cardioprotective efficacy of zoniporide in a model of myocardial preservation - the rat isolated working heart. British journal of pharmacology. 2011 Feb;162(3):633-47.
- [2]. Marala RB, et al. Zoniporide: a potent and highly selective inhibitor of human Na(+)/H(+) exchanger-1. European journal of pharmacology. 2002 Sep 06;451(1):37-41. [Content Brief]
- [3]. Guzman-Perez A, et al. Discovery of zoniporide: a potent and selective sodium-hydrogen exchanger type 1 (NHE-1) inhibitor with high aqueous solubility. Bioorganic & medicinal chemistry letters. 2001 Mar 26;11(6):803-7. [Content Brief]
- [4]. Clements-Jewery H, et al. Cardioprotective efficacy of zoniporide, a potent and selective inhibitor of Na+/H+ exchanger isoform 1, in an experimental model of cardiopulmonary bypass. British journal of pharmacology. 2004 May;142(1):57-66.
- [5]. Watson AJ, et al. Enhanced preservation of pig cardiac allografts by combining erythropoietin with glyceryl trinitrate and zoniporide. American journal of transplantation : official journal of the American Society of Transplantation and the American Society of Transplant Surgeons. 2013 Jul;13(7):1676-87.
Keywords
