CAS NO: | 176644-21-6 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Cas No. | 176644-21-6 |
别名 | N-(二氨基亚甲基)-2-甲基-5-(甲基磺酰基)-4-(1H-吡咯-1-基)苯甲酰胺 |
化学名 | 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 |
分子式 | C14H16N4O3S |
分子量 | 320.4 |
溶解度 | ≤5mg/ml in DMSO;20mg/ml in dimethyl formamide |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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: |