| 靶点: |
PD173212 is a selective N-type voltage sensitive calcium channel (VSCC) blocker, with an IC50 of 36 nM in IMR-32 assays. |
| 体外研究: |
PD173212 (PD 173212, 300 nM) potently blocks recombinant B-class (N-type) calcium channel currents 78±7.8%, with an IC50 of 74 nM, by whole-cell voltage-clamp techniques. PD 173212 possesses selectivity for non L-type Ca2+ channels versus neuronal Na+, K+, and L-type Ca2+ channels. |
| 体内研究: |
PD173212 (30 mg/kg, i.v.) shows moderate efficacy in preventing tonic seizures in the audiogenic seizure model. |
| 参考文献: |
[1]. Hu LY, et al. Structure-activity relationship of N-methyl-N-aralkyl-peptidylamines as novel N-type calcium channel blockers. Bioorg Med Chem Lett. 1999 Aug 2;9(15):2151-6. |
| 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 |
1.667 ml |
8.335 ml |
16.671 ml |
| 5 mM |
0.333 ml |
1.667 ml |
3.334 ml |
| 10 mM |
0.167 ml |
0.834 ml |
1.667 ml |
| 50 mM |
0.033 ml |
0.167 ml |
0.333 ml |
|
| 注意: |
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