产品描述: | GV-58 is a novel N- and P/Q-type calcium (Ca2+) channel agonist with EC50s of 7.21 and 8.81 μM, respectively. GV-58 slows the deactivation of channels, resulting in a large increase in presynaptic Ca2+ entry during activity. GV-58 can be used in lambert-eaton myasthenic syndrome (LEMS) research |
靶点: |
N-type calcium channel:7.21 μM (EC50);P/Q-type calcium channel:8.81 μM (EC50);CalciumChannel |
体外研究: |
GV-58 (50 μM; 30 min) restores function in LEMS passive transfer neuromuscular junction. Cell Viability Assay Cell Line: Upper arm muscle isolated from LEMS mice Concentration: 50 μM Incubation Time: 30 min Result: Increased the mEPP frequency from 3.27 s−1 in vehicle controls to 10.45 s−1.Showed a slight facilitation followed by depression to ∼94% at the final EPP in the train. |
参考文献: |
1. Tarr TB, et al. Evaluation of a novel calcium channel agonist for therapeutic potential in Lambert-Eaton myasthenic syndrome. J Neurosci. 2013 Jun 19;33(25):10559-67. 2. Tarr TB, et al. Complete reversal of Lambert-Eaton myasthenic syndrome synaptic impairment by the combined use of a K+ channel blocker and a Ca2+ channel agonist. J Physiol. 2014 Aug 15;592(16):3687-96. 3. Meriney SD, et al. Lambert-Eaton myasthenic syndrome: mouse passive-transfer model illuminates disease pathology and facilitates testing therapeutic leads. Ann N Y Acad Sci. 2018 Jan;1412(1):73-81. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.67 ml |
13.351 ml |
26.702 ml |
5 mM |
0.534 ml |
2.67 ml |
5.34 ml |
10 mM |
0.267 ml |
1.335 ml |
2.67 ml |
50 mM |
0.053 ml |
0.267 ml |
0.534 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。 |