| 产品描述： | Rimeporide (EMD-87580) is a potent and selective Sodium hydrogen exchange 1 (NHE-1) inhibitor. |
| 靶点： |
Sodium Channel |
| 细胞实验： |
To induce hypertrophy, myocytes were treated for 10 min or 24 h as appropriate and noted under Results with 10 μM phenylephrine in the absence or presence of the following agents: the NHE-1 inhibitor EMD87580 (5 μM) or cariporide (5 μM), the JNK1/2 inhibitor SP600125, the p38 inhibitor SB203580, the ERK1/2 inhibitor PD98059 (all at 10 μM), and the reverse mode Na+-Ca2+ exchange inhibitor KB-R7943 or SN-6 (both at 10 μM). All drugs were added 30 min before the addition of phenylephrine |
| 动物实验： |
Two groups were studied. The treatment group (n = 5) received EMD 87580 at a dose of 5 mg/kg IV bolus 5 min before aortic cross-clamping and 10 mol/L EMD 87580 in the cardioplegic solution. The control group (n = 9) received the same volume of saline vehicle. Systemic pretreatment was used to ensure drug availability during the ischemic period prior to CPA. Direct infusion via cardioplegia ensures drug delivery at the time of ischemia (CPA), and it decreases the variability of drug delivery that may occur during the hemodilution with CPB initiation. Incorporation into the cardioplegia also minimizes the potential variable of drug/extracorporeal circuit interactions. Using this dosing regimen, the plasma concentration of EMD 87580 was in the 2,500 to 3,000 ng/mL range at 10 min after CPB. This concentration has been shown to be effective at Na+/H+ exchanger inhibition in vitro |
| 参考文献： |
1. Stanbouly S, et al. Sodium hydrogen exchange 1 (NHE-1) regulates connexin 43 expression in cardiomyocytes via reverse mode sodium calcium exchange and c-Jun NH2-terminal kinase-dependent pathways. J Pharmacol Exp Ther. 2008 Oct;327(1):105-13. 2. Cox CS Jr, et al. Improved myocardial function using a Na+/H+ exchanger inhibitor during cardioplegic arrest and cardiopulmonary bypass. Chest. 2003 Jan;123(1):187-94. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3 ml |
14.998 ml |
29.996 ml |
| 5 mM |
0.6 ml |
3 ml |
5.999 ml |
| 10 mM |
0.3 ml |
1.5 ml |
3 ml |
| 50 mM |
0.06 ml |
0.3 ml |
0.6 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京