| 产品描述: | Bepridil is a calcium channel blocker and also inhibits Na+/Ca2+ exchange (NCX), sodium channels and cardiac sarcolemmal KATP channels. |
| 靶点: |
Calcium Channel;CalciumChannel |
| 体外研究: |
Bepridil (1-100 microM) inhibited the K(ATP) channel current in a concentration-dependent manner. The IC(50) value of bepridil was estimated to be 10.5 microM for outward K(ATP) channel currents (holding potential, +60 mV) and 6.6 microM for inward K(ATP) channel currents (holding potential, -60 mV). Bepridil (0.1-30 microM) also inhibited K(Na) channel currents measured at the holding potential of -60 mV, in a concentration-dependent manner with an IC(50) value of 2.2 microM |
| 体内研究: |
The predominant effects of Bepridil (cumulative dose = 9.0 mg/kg i.v.) in the conscious rat were reduced coronary vascular resistance and heart rate. Bepridil showed selectivity for the coronary circulation since systemic vascular resistance was not significantly reduced until cumulative i.v. dosage of 21.0 mg/kg was administered |
| 参考文献: |
1. Flaim SF, et al. Effects of bepridil hydrochloride on cardiocirculatory dynamics, coronary vascular resistance, and cardiac output distribution in normal, conscious rats. J Cardiovasc Pharmacol. 1988 Mar;11(3):363-72. 2. Li Y, et al. Bepridil blunts the shortening of action potential duration caused by metabolic inhibition via blockade of ATP-sensitive K(+) channels and Na(+)-activated K(+) channels. J Pharmacol Exp Ther. 1999 Nov;291(2):562-8. 3. Qiu M, Li Z, Chen Y, et al. Tolcapone Potently Inhibits Seminal Amyloid Fibrils Formation and Blocks Entry of Ebola Pseudoviruses. Frontiers in Microbiology. 2020, 11: 504. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.481 ml |
12.407 ml |
24.814 ml |
| 5 mM |
0.496 ml |
2.481 ml |
4.963 ml |
| 10 mM |
0.248 ml |
1.241 ml |
2.481 ml |
| 50 mM |
0.05 ml |
0.248 ml |
0.496 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。 |