| 产品描述: | Mibefradil dihydrochloride is an blocker of calcium channel with moderate selectivity for T-type Ca2+ channels (T-type and L-type currents with IC50s of 2.7 μM and 18.6 μM, respectively). |
| 靶点: |
Calcium Channel;CalciumChannel |
| 体内研究: |
Compared with the saline-treated group, rats receiving Mibefradil or Ethosuximide show significant lower CaV3.2 expression in the spinal cord and DRG. |
| 细胞实验: |
Human Orai1-3 cDNAs in tetracycline-regulated pcDNA4/TO vectors were transfected into HEK293 T-REx cells with stromal interaction molecule 1 (STIM1) stable expression. The Orai currents were recorded by whole-cell and excised-membrane patch clamp. Ca2+influx or release was measured by Fura-PE3/AM. Cell growth and death were monitored by WST-1, LDH assays and flow cytometry |
| 参考文献: |
1. Shiue SJ, et al. Chronic intrathecal infusion of T-type calcium channel blockers attenuates CaV3.2 upregulation in nerve-ligated rats. Acta Anaesthesiol Taiwan. 2016 Oct 17. pii: S1875-4597(16)30071-6. 2. Li P , Rubaiy H N , Gui‐Lan Chen, et al. Mibefradil, a T‐type Ca2+ channel blocker also blocks Orai channels by action at the extracellular surface[J]. British Journal of Pharmacology, 2019, 176. 3. Brain KL, et al. The sources and sequestration of Ca(2+) contributing to neuroeffector Ca(2+) transients in the mouse vas deferens. J Physiol. 2003 Dec 1;553(Pt 2):627-35. 4. Yu YF, et al. Protection of the cochlear hair cells in adult C57BL/6J mice by T-type calcium channel blockers. Exp Ther Med. 2016 Mar;11(3):1039-1044. |
| 溶解性: |
Soluble in H2O |
| 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 |
1.759 ml |
8.794 ml |
17.589 ml |
| 5 mM |
0.352 ml |
1.759 ml |
3.518 ml |
| 10 mM |
0.176 ml |
0.879 ml |
1.759 ml |
| 50 mM |
0.035 ml |
0.176 ml |
0.352 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。 |