| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Eniporide targets the Na+/H+ exchanger isoform 1 (NHE-1). This is a membrane transporter protein that plays a crucial role in cellular pH regulation by exchanging intracellular H+ for extracellular Na+. NHE-1 is the predominant isoform in cardiac myocytes and is implicated in various pathophysiological conditions, particularly myocardial ischemia and reperfusion injury. By specifically inhibiting NHE-1, eniporide modulates intracellular pH and sodium levels, thereby protecting the heart from ischemic injury.
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| ln Vitro |
ENIPORIDE is a Na+/H+ exchange reagent that works well.
In vitro, eniporide inhibits NHE-1-mediated Na+/H+ exchange. Studies have shown that blocking NHE with eniporide reduces ischemic Na+ overload and improves post-ischemic contractile recovery in isolated hearts. Compared to other NHE blockers like EIPA, eniporide is more effective and exhibits fewer side effects. These in vitro findings demonstrate its potent and specific NHE-1 inhibitory activity and its cardioprotective potential. |
| ln Vivo |
Following ischemia/reperfusion brought on by crystalloid cardiac arrest, eniporide (3 mg/kg; intravenous injection; systemic infusion prior to cardiac arrest) increases function and high-energy phosphate content in healthy pig hearts [1].
In vivo, eniporide has been shown to limit infarct size in various animal models of myocardial ischemia and reperfusion. It improves cardiac performance depression associated with myocardial ischemia/reperfusion. In a clinically relevant porcine model of cardiopulmonary bypass and cardiac arrest, eniporide modulates cardiac performance and high-energy phosphate content. These in vivo findings support its potential as a cardioprotective agent for the treatment of acute myocardial infarction. |
| Enzyme Assay |
The in vitro enzyme/receptor binding (non-cellular) assay for eniporide typically measures its ability to inhibit Na+/H+ exchange activity in membrane preparations. These assays use isolated membrane vesicles or cells expressing NHE-1 and measure the pH-dependent uptake of radiolabeled Na+ or the recovery of intracellular pH after an acid load. The compound's inhibitory potency is determined by measuring the reduction in Na+/H+ exchange activity. These assays provide a direct measure of the compound's NHE-1 inhibitory activity.
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| Cell Assay |
In vitro cellular assays for eniporide assess its ability to inhibit NHE-1-mediated intracellular pH regulation. Cells expressing NHE-1 are loaded with a pH-sensitive fluorescent dye, and intracellular pH is monitored after an acid load. The compound's ability to inhibit the recovery of intracellular pH is measured. Alternatively, Na+ uptake can be measured using radiolabeled Na+. These assays demonstrate the compound's functional inhibition of NHE-1 in a relevant cellular context.
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| Animal Protocol |
Animal/Disease Models: Clinically relevant porcine cardiopulmonary bypass (CPB) and cardioplegia model [1]
Doses: 3 mg/kg Route of Administration: intravenous (iv) (iv)injection; whether to add 2 μM to systemic infusion before cardioplegia Ennipoli Experimental Results: versus standard blood Flow dynamics (including vascular pressure and cardiac index) and cardiac functional factors had no effect. Reduce myocardial edema and improve heart function. In vivo animal studies for eniporide have been conducted in various models of myocardial ischemia and reperfusion. These include rat, pig, and other animal models. In these studies, eniporide is typically administered before the onset of ischemia, and endpoints include infarct size, cardiac performance, and high-energy phosphate content. The compound's ability to limit infarct size and improve cardiac function has been demonstrated in these models, supporting its potential as a cardioprotective agent. |
| ADME/Pharmacokinetics |
Specific pharmacokinetic data for Eniporide are not extensively detailed in the available literature. However, as a small molecule NHE-1 inhibitor, its pharmacokinetic properties would be typical of this class of compounds. The compound was evaluated in clinical trials, indicating that it has suitable pharmacokinetic properties for human use. However, the specific parameters such as half-life, Cmax, and bioavailability are not provided.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Eniporide are not extensively detailed in the available literature. As a NHE-1 inhibitor, its toxicity profile is likely related to its mechanism of action, potentially affecting other tissues where NHE-1 is expressed. However, preclinical toxicology studies would have been conducted as part of its development. The compound was evaluated in clinical trials for acute myocardial infarction, where its safety would have been assessed. However, these clinical trials did not demonstrate efficacy in limiting infarct size in patients.
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| References |
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| Additional Infomation |
Eniporide is a specific NHE-1 inhibitor that was developed for the treatment of myocardial ischemia-reperfusion injury. Extensive preclinical studies demonstrated its efficacy in limiting infarct size in various animal models. However, clinical trials, such as the evaluation of eniporide as an adjunct to early reperfusion therapy for acute myocardial infarction, did not demonstrate efficacy in limiting infarct size or improving clinical outcomes in patients. As a result, eniporide did not advance to become a clinically approved therapeutic agent. It remains a research tool for studying NHE-1 function.
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| Molecular Formula |
C14H16N4O3S
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|---|---|
| Molecular Weight |
320.367
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| Exact Mass |
320.094
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| CAS # |
176644-21-6
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| Related CAS # |
Eniporide hydrochloride;211813-86-4
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| PubChem CID |
6433092
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
635.9±65.0 °C at 760 mmHg
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| Flash Point |
338.4±34.3 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.656
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| LogP |
0.38
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
545
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C([H])([H])[H])(C1C([H])=C(C(/N=C(\N([H])[H])/N([H])[H])=O)C(C([H])([H])[H])=C([H])C=1N1C([H])=C([H])C([H])=C1[H])(=O)=O
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| InChi Key |
UADMBZFZZOBWBB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H16N4O3S/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)
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| Chemical Name |
N-(diaminomethylidene)-2-methyl-5-methylsulfonyl-4-pyrrol-1-ylbenzamide
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1214 mL | 15.6070 mL | 31.2139 mL | |
| 5 mM | 0.6243 mL | 3.1214 mL | 6.2428 mL | |
| 10 mM | 0.3121 mL | 1.5607 mL | 3.1214 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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