Eniporide
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 320.4 |
Cas No. | 176644-21-6 |
Formula | C14H16N4O3S |
Solubility | ≤5mg/ml in DMSO;20mg/ml in dimethyl formamide |
Chemical Name | N-(aminoiminomethyl)-2-methyl-5-(methylsulfonyl)-4-(1H-pyrrol-1-yl)-benzamide |
SDF | Download SDF |
Canonical SMILES | CC1=C(C(NC(N)=N)=O)C=C(S(C)(=O)=O)C(N2C=CC=C2)=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |