Eniporide |
Catalog No.GC16924
One-Click Copy Product Info
|
Na+/H+ exchange inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 176644-21-6
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
IC50: 4.7 nM
Eniporide is a Na+/H+ exchange inhibitor.
Regulation of intracellular pH is a very complex process and reflects a net balance of alkalinizing and acidification processes. The Na+-H+ exchange plays a critical role in the regulation of intracellular pH by removing protons.
In vitro: Eniporide was identified as a selective inhibitor of Na+-H+ exchange and a compound of the benzoylguanidine group. In addition, eniporide and its metabolite were found to inhibit the Na+-H+ exchange in acidified rabbit erythrocytes with an IC50 value of 4.7 ± 0.6 and 15 ± 3 nM, respectively [1].
In vivo: Animal study showed that the pretreatment of the mice with the eniporide led to a substantial decrease of annexin-V–positive cardiomyocytes in the I/R 30/90 group from 20.2% to 2.2%. Moreover, the pretreatment of I/R 30/90 mice with eniporide resulted in the complete absence of IgG-positive cells, suggesting that the cardiomyocytes with extensive cell membrane leakage were a result of an active cell death program [2].
Clinical trial: Clinical pharmacokinetic-pharmacodynamic evaluation of eniporide with platelet swelling time as a biomarker has been reported. Eniporide showed linear pharmacokinetics with an average half-life of 2 hours. The mean total body clearance and volume of distribution were 34.4 L/h and 77.5 L, respectively. An average of 43% of the dose was recovered unchanged from urine [1].
References:
[1] Bhattaram VA, Nagaraja NV, Peters T, Machnig T, Kroesser S, Kovar A, Derendorf H. Population pharmacokinetics of eniporide and its metabolite in healthy subjects and patients with acute myocardial infarction. J Clin Pharmacol. 2005 Jun;45(6):631-9.
[2] Dumont EA et al. Cardiomyocyte death induced by myocardial ischemia and reperfusion: measurement with recombinant human annexin-V in a mouse model. Circulation. 2000 Sep 26;102(13):1564-8.
| Cas No. | 176644-21-6 | SDF | |
| Chemical Name | N-(aminoiminomethyl)-2-methyl-5-(methylsulfonyl)-4-(1H-pyrrol-1-yl)-benzamide | ||
| Canonical SMILES | CC1=C(C(NC(N)=N)=O)C=C(S(C)(=O)=O)C(N2C=CC=C2)=C1 | ||
| Formula | C14H16N4O3S | M.Wt | 320.4 |
| Solubility | ≤5mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.1211 mL | 15.6055 mL | 31.211 mL |
| 5 mM | 624.2 μL | 3.1211 mL | 6.2422 mL |
| 10 mM | 312.1 μL | 1.5605 mL | 3.1211 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)