Zoniporide
Based on 2 publication(s) in Google Scholar
Zoniporide (CP-597396) 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 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 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.
- Purity: 99.89%
- CAS No.: 241800-98-6
- Formula: C17H16N6O
- Molecular Weight:320.35
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Zoniporide
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Biological Activity
Description
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Rat NHE1 67-73 nM (IC50) |
Human NHE-1 59 nM (IC50) |
ERK1 |
ERK2 |
STAT3 |
In Vitro
Zoniporide (CP-597396) (1 nM‑100 μM; 6 min) 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) 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) 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) potently inhibits endogenous NHE-1-mediated swelling in human platelet-rich plasma with an IC50 of 0.059 μM[2].
Zoniporide (compound 3d) 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) 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) 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.
Parmacokinetics
In Vivo
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. 241800-98-6
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Appearance Solid
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Molecular Weight 320.35
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Formula C17H16N6O
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Color White to off-white
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SMILES
N=C(N)NC(C1=C(C2CC2)N(C3=C4C(N=CC=C4)=CC=C3)N=C1)=O
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Synonyms
CP-597396
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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
Solvent & Solubility
In Vitro:
DMSO : 125 mg/mL (390.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (301 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.1216 mL | 15.6079 mL | 31.2159 mL | 78.0396 mL |
| 5 mM | 0.6243 mL | 3.1216 mL | 6.2432 mL | 15.6079 mL | |
| 10 mM | 0.3122 mL | 1.5608 mL | 3.1216 mL | 7.8040 mL | |
| 15 mM | 0.2081 mL | 1.0405 mL | 2.0811 mL | 5.2026 mL | |
| 20 mM | 0.1561 mL | 0.7804 mL | 1.5608 mL | 3.9020 mL | |
| 25 mM | 0.1249 mL | 0.6243 mL | 1.2486 mL | 3.1216 mL | |
| 30 mM | 0.1041 mL | 0.5203 mL | 1.0405 mL | 2.6013 mL | |
| 40 mM | 0.0780 mL | 0.3902 mL | 0.7804 mL | 1.9510 mL | |
| 50 mM | 0.0624 mL | 0.3122 mL | 0.6243 mL | 1.5608 mL | |
| 60 mM | 0.0520 mL | 0.2601 mL | 0.5203 mL | 1.3007 mL | |
| 80 mM | 0.0390 mL | 0.1951 mL | 0.3902 mL | 0.9755 mL | |
| 100 mM | 0.0312 mL | 0.1561 mL | 0.3122 mL | 0.7804 mL |
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