Zoniporide dihydrochloride
Based on 2 publication(s) in Google Scholar
Zoniporide dihydrochloride (CP-597396 dihydrochloride) 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 dihydrochloride 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 dihydrochloride is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury.
For research use only. We do not sell to patients.
- CAS No.: 241799-10-0
- Formula: C17H18Cl2N6O
- Molecular Weight:393.27
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Zoniporide dihydrochloride
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Biological Activity
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Rat NHE1 67-73 nM (IC50) |
Human NHE-1 59 nM (IC50) |
ERK1 |
ERK2 |
STAT3 |
Zoniporide (1 nM‑100 μM; 6 min) dihydrochloride (CP-597396 dihydrochloride) potently inhibits human NHE-1-mediated 22Na+ uptake in PS120 fibroblast cells with an IC50 of 14 nM[2].
Zoniporide (1 nM‑100 μM; 6 min) dihydrochloride inhibits human NHE-2-mediated 22Na+ uptake in PS120 fibroblast cells with an IC50 of 2.2 μM, showing 157-fold lower potency than for human NHE-1[2].
Zoniporide (1 nM‑100 μM; 6 min) dihydrochloride inhibits rat NHE-3-mediated 22Na+ uptake in PS120 fibroblast cells with an IC50 of 220 μM, showing 15,700-fold lower potency than for human NHE-1[2].
Zoniporide (1 nM‑100 μM) dihydrochloride potently inhibits endogenous NHE-1-mediated swelling in human platelet-rich plasma with an IC50 of 0.059 μM[2].
Zoniporide (compound 3d) dihydrochloride potently and selectively inhibits human NHE-1 (IC50 = 59 nM) in transfected fibroblasts[3].
Zoniporide (0.001-1.0 μM; 8 min at 25°C; 0.01-1.0 μM; 8 min at 37°C) dihydrochloride potently inhibits native NHE1 activity in adult rat ventricular myocytes with an IC50 of 73 nM at 25°C, and retains comparable inhibitory potency at 37°C[4].
Zoniporide (0.001-1.0 μM; 5 min) dihydrochloride potently inhibits native NHE1 activity in adult rat platelets with an IC50 of 67 nM[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Landrace (juvenile, 40-60 kg, mixed gender, orthotopic heart transplantation with donor brain death induced by subdural Foley catheter balloon inflation, ~260 minutes total ischemic time)[5]
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Dosage:1 mM
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Administration:Added to Celsior solution for donor cardiac arrest and cold storage
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Result:Achieved 40% successful cardiopulmonary bypass weaning rate in combination with glyceryl trinitrate; post-transplant left ventricular minute work, cardiac output, and mean arterial pressure remained at less than half the baseline value, and decreased stroke work index by 12% at 3.25 hours post-weaning.
Achieved 80% successful cardiopulmonary bypass weaning rate in combination with erythropoietin and glyceryl trinitrate; post-transplant left ventricular minute work, cardiac output, and mean arterial pressure remained similar to baseline values, and increased stroke work index by 30% at 3.25 hours post-weaning.
Resulted in plasma cardiac troponin I levels of 60.3 μg/L at 1 hour post-reperfusion, 128.8 μg/L at 2 hours post-reperfusion, and 206.2 μg/L at 3 hours post-reperfusion in combination with erythropoietin and glyceryl trinitrate, which were lower than levels in the group receiving zoniporide plus glyceryl trinitrate at all corresponding time points.
Chemical Information
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CAS No. 241799-10-0
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Molecular Weight 393.27
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Formula C17H18Cl2N6O
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SMILES
N=C(N)NC(C1=C(C2CC2)N(C3=C4C(N=CC=C4)=CC=C3)N=C1)=O.[H]Cl.[H]Cl
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Synonyms
CP-597396 dihydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Carbohydr Polym
Slc9a1 plays a vital role in chitosan oligosaccharide transport across the intestinal mucosa of mice. [Abstract]2023 Jan 1:299:120179. PMID: 36876794 -
J Biol Chem
Type 2 diabetic mice enter a state of spontaneous hibernation-like suspended animation following accumulation of uric acid. [Abstract]2021 Oct;297(4):101166. PMID: 34487763
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)