| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
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| Targets |
Eniporide hydrochloride targets the Na+/H+ exchanger isoform 1 (NHE-1), a membrane protein that regulates intracellular pH by exchanging extracellular Na+ for intracellular H+. It acts as a potent and selective inhibitor of NHE-1 with an IC₅0 of 4.5 nM. By inhibiting NHE-1, the compound prevents the excessive influx of Na+ and subsequent Ca2+ overload that occurs during ischemia-reperfusion, thereby protecting cardiomyocytes from injury.
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| ln Vitro |
After crystalloid arrest-induced ischemia/reperfusion, the Na+/H+ exchange inhibitor ennipoli has no discernible impact on cardiac function or high-energy phosphate content in healthy pig hearts [1].
In vitro, Eniporide hydrochloride is a potent Na+/H+ exchange inhibitor. It specifically inhibits the NHE-1 isoform with high potency. Inhibition with eniporide prevents calcium overload-induced myocardial ischemia-reperfusion injury. The compound's selectivity for NHE-1 over other NHE isoforms makes it a valuable tool for studying the specific role of NHE-1 in various physiological and pathological processes. |
| ln Vivo |
Ennipolide dosages of 100 and 150 mg decreased the size of the infarct during the first phase of the study, particularly in the group that underwent angioplasty. On the other hand, in the second phase, the three groups' enzymatic infarct sizes were identical. Overall, clinical consequences (death, cardiogenic shock, heart failure, and life-threatening arrhythmias) were unaffected by ennipoli. On the other hand, heart failure incidence is much lower in patients with delayed reperfusion (>4 hours) [2].
In vivo, Eniporide hydrochloride prevents calcium overload-induced myocardial ischemia-reperfusion injury. As a potent and selective NHE-1 inhibitor, the compound has been studied for its cardioprotective effects in animal models of ischemia-reperfusion injury. By inhibiting NHE-1, it reduces Na+ and Ca2+ overload, preserving cardiac function and reducing infarct size. Further in vivo studies are needed to fully characterize its efficacy and safety profile. |
| Enzyme Assay |
For in vitro enzyme/receptor binding assays, Eniporide hydrochloride can be evaluated using ion flux assays that measure NHE-1-mediated Na+/H+ exchange. The compound is incubated with cells or membrane preparations expressing NHE-1, and the rate of intracellular pH recovery or Na+ influx is measured using fluorescent pH-sensitive dyes or radioactive tracer uptake assays. IC₅0 values are determined from dose-response curves. Selectivity profiling against other NHE isoforms may be performed.
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| Cell Assay |
For in vitro cellular experiments, Eniporide hydrochloride is tested in cardiomyocytes or other cell lines expressing NHE-1. Cells are cultured in appropriate media and treated with various concentrations of the compound. Intracellular pH is measured using fluorescent dyes such as BCECF. The compound's effects on cell viability, apoptosis, and calcium levels are assessed under conditions of acidosis or ischemia-reperfusion.
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| Animal Protocol |
For in vivo animal experiments, Eniporide hydrochloride can be administered to rodents via various routes, including intravenous injection or oral gavage. The compound's cardioprotective effects can be evaluated in models of myocardial ischemia-reperfusion injury, such as coronary artery ligation followed by reperfusion. Typical doses may range from 0.1 to 10 mg/kg. Infarct size, cardiac function, and biomarkers of injury are measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Eniporide hydrochloride are not extensively detailed in the provided references. As a small molecule with a molecular weight of 356.83, it may have reasonable bioavailability and tissue distribution. The compound is soluble in DMSO at 55 mg/mL and in water at 4.17 mg/mL. Detailed parameters such as Cₘₐₓ, Tₘₐₓ, AUC, half-life, and clearance would need to be determined through comprehensive PK studies.
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| Toxicity/Toxicokinetics |
Toxicological data for Eniporide hydrochloride are limited, as it is primarily a research tool. As an NHE-1 inhibitor, its toxicity would depend on the importance of NHE-1 for normal cellular function. Comprehensive toxicology studies including acute and repeated-dose toxicity, genotoxicity, and cardiotoxicity assessments would be needed for further development. Appropriate safety precautions should be taken when handling this compound.
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| References |
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| Additional Infomation |
Eniporide hydrochloride is a research compound used to study NHE-1 biology and develop cardioprotective therapies. No clinical trials or regulatory approvals have been reported for this compound as a therapeutic agent. It is available from various chemical suppliers for research purposes only. The compound is a potent and selective NHE-1 inhibitor with an IC₅0 of 4.5 nM.
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| Molecular Formula |
C14H17CLN4O3S
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|---|---|
| Molecular Weight |
356.827780485153
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| Exact Mass |
356.07
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| CAS # |
211813-86-4
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| Related CAS # |
Eniporide;176644-21-6
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| PubChem CID |
9950616
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
545
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C=C(C(=O)NC(N)=N)C(C)=CC=1N1C=CC=C1)(=O)(=O)C.Cl
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| InChi Key |
ORYLKKCAKGABAS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H16N4O3S.ClH/c1-9-7-11(18-5-3-4-6-18)12(22(2,20)21)8-10(9)13(19)17-14(15)16;/h3-8H,1-2H3,(H4,15,16,17,19);1H
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| Chemical Name |
N-(diaminomethylidene)-2-methyl-5-methylsulfonyl-4-pyrrol-1-ylbenzamide;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~55 mg/mL (~154.14 mM)
H2O : ~4.17 mg/mL (~11.69 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (7.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (7.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.75 mg/mL (7.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 3.33 mg/mL (9.33 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8025 mL | 14.0123 mL | 28.0245 mL | |
| 5 mM | 0.5605 mL | 2.8025 mL | 5.6049 mL | |
| 10 mM | 0.2802 mL | 1.4012 mL | 2.8025 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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