Zoniporide mesylate
Based on 2 publication(s) in Google Scholar
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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- CAS 番号: 249296-45-5
- 分子式: C18H20N6O4S
- 分子量:416.45
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
MedChemExpress(MCE)の使用を引用している文献 Zoniporide mesylate
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生物活性
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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) mesylate (CP-597396 mesylate) 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) mesylate 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) mesylate 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) mesylate potently inhibits endogenous NHE-1-mediated swelling in human platelet-rich plasma with an IC50 of 0.059 μM[2].
Zoniporide (compound 3d) mesylate 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) mesylate 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) mesylate 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.
化学情報
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CAS 番号 249296-45-5
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分子量 416.45
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分子式 C18H20N6O4S
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SMILES
N=C(N)NC(C1=C(C2CC2)N(C3=C4C(N=CC=C4)=CC=C3)N=C1)=O.CS(=O)(O)=O
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別名
CP-597396 mesylate
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)