| Identification | Back Directory | [Name]
ENIPORIDE | [CAS]
176644-21-6 | [Synonyms]
CS-1941
CS-1337
ENIPORID
ENIPORIDE
EMD 96785
EMD 96785,ENIPORIDE
EMD-96785;EMD 96785
Eniporide(EMD96785)
N-Carbamimidoyl-2-methyl-5-(methylsulfonyl)
N-(diaMinoMethylidene)-2-Methyl-5-Methylsulfonyl-4-pyrrol-1-ylbenzaMide
N-CarbaMiMidoyl-2-Methyl-5-(Methylsulfonyl)-4-(1H-pyrrol-1-yl)benzaMide
N-(Aminoiminomethyl)-2-methyl-5-(methylsulfonyl)-4-(1H-pyrrol-1-yl)benzamide
N-(Diaminomethylene)-2-methyl-5-(methylsulfonyl)-4-(1H-pyrrol-1-yl)benzamide
Benzamide, N-(aminoiminomethyl)-2-methyl-5-(methylsulfonyl)-4-(1H-pyrrol-1-yl)- | [Molecular Formula]
C14H16N4O3S | [MDL Number]
MFCD08690425 | [MOL File]
176644-21-6.mol | [Molecular Weight]
320.37 |
| Chemical Properties | Back Directory | [density ]
1.41±0.1 g/cm3(Predicted) | [storage temp. ]
under inert gas (nitrogen or Argon) at 2–8 °C | [solubility ]
≤5mg/ml in DMSO;20mg/ml in dimethyl formamide | [form ]
crystalline solid | [pka]
10.63±0.46(Predicted) |
| Hazard Information | Back Directory | [Description]
Eniporide is a selective inhibitor of human Na+/H+ exchanger isoform 1 (NHE-1) (IC50 = 4.5 nM). Inhibition with eniporide prevents calcium overload-induced myocardial ischemia-reperfusion injury in vitro and in vivo. | [Uses]
Eniporide (EMD 96785) is a Na(+)/H(+) exchange (NHE) inhibitor. Eniporide specifically inhibits the NHE-1 isoform. Eniporide improves cardiac performance inhibition associated with myocardial ischemia/reperfusion in animals, and limits infarct size in experimental models. Eniporide regulates cardiac performance and high-energy phosphate content in clinically relevant pig models of CPB and cardiac arrest[1][2]. | [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]. | [IC 50]
4.7 nm | [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. |
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BOC Sciences
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www.bocsci.com |
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