| 产品描述: | CLP290 is an activator of the neuron-specific K+-Cl cotransporter KCC2 and displays potential for the treatment of a wide range of neurological and psychiatric indications. |
| 靶点: |
Potassium Channel |
| 体内研究: |
In vivo co-treatment with morphine and oral CLP290 prevented membrane KCC2 downregulation in SDH neurons.Concurrently, co-treatment with CLP290 significantly mitigated MIH and acute administration of CLP257 in established MIH restored normal nociceptive behavior. |
| 动物实验: |
Morphine sulfate (50 mg/ml) was diluted in saline sterile solution immediately before injection.?Morphine or saline were subcutaneously injected twice a day (10 mg/kg;?9 a.m. 6 p.m.) in na?ve adult rats.The KCC2 enhancer CLP257 and its carbamate pro-drug CLP290 were freshly diluted in 20% 2-hydroxypropyl-β-cyclodextrin (HPCD) prior injection.CLP257 or vehicle were delivered intraperitoneally after 7 8 days of morphine or saline, as described (100 mg/kg).?CLP290 or vehicle were delivered orally by gavage twice a day for the whole duration of the morphine/saline treatment (100 mg/kg). |
| 参考文献: |
1. Ferrini F, et al. Enhancing KCC2 function counteracts morphine-induced hyperalgesia. Sci Rep. 2017 Jun 20;7(1):3870. |
| 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 |
2.472 ml |
12.362 ml |
24.724 ml |
| 5 mM |
0.494 ml |
2.472 ml |
4.945 ml |
| 10 mM |
0.247 ml |
1.236 ml |
2.472 ml |
| 50 mM |
0.049 ml |
0.247 ml |
0.494 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。 |