Zoniporide hydrochloride
Based on 2 publication(s) in Google Scholar
Zoniporide hydrochloride (CP-597396 hydrochloride) 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 hydrochloride 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 hydrochloride 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.: 241800-97-5
- Formula: C17H17ClN6O
- Molecular Weight:356.81
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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 hydrochloride
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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 (1 nM‑100 μM; 6 min) hydrochloride 可抑制 PS120 成纤维细胞中由人源 NHE-2 介导的 22Na+ 摄取,其 IC50 为 2.2 μM,效力比对人源 NHE-1 的作用低 157 倍[2]。
Zoniporide (1 nM‑100 μM; 6 min) hydrochloride 可抑制 PS120 成纤维细胞中大鼠 NHE-3 介导的 22Na+ 摄取,其 IC50 为 220 μM,效力较人源 NHE-1 低 15700 倍[2]。
Zoniporide (1 nM‑100 μM) hydrochloride 可强效抑制富血小板血浆中内源性 NHE-1 介导的肿胀作用,其 IC50 为 0.059 μM[2]。
Zoniporide (compound 3d) hydrochloride 可在转染的成纤维细胞中强效且选择性地抑制人源 NHE-1 (IC50 = 59 nM)[3]。
Zoniporide (0.001-1.0 μM; 8 min at 25°C; 0.01-1.0 μM; 8 min at 37°C) hydrochloride 可强效抑制成年大鼠心室肌细胞中的天然 NHE1 活性,在 25°C 条件下其 IC50 为 73 nM,且在 37°C 条件下仍保持相当的抑制效力[4]。
Zoniporide (0.001-1.0 μM; 5 min) hydrochloride 可强效抑制成年大鼠血小板中天然 NHE1 的活性,其 IC50 为 67 nM[4]。
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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. 241800-97-5
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Molecular Weight 356.81
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Formula C17H17ClN6O
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SMILES
O=C(C1=C(C2CC2)N(C3=C4C=CC=NC4=CC=C3)N=C1)NC(N)=N.[H]Cl
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Synonyms
CP-597396 hydrochloride
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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]
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)