S82166 |
Mibefradil dihydrochloride |
源叶(MedMol) | ≥98% |
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- 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: -20℃;充氩;干燥
- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)