| 产品描述： | VU 0240551 is a potent neuronal K-Cl cotransporter KCC2 inhibitor (IC50=560 nM) and is selective versus NKCC1. VU 0240551 also inhibits hERG and L-type Ca2+ channels. VU 0240551 attenuates GABA-induced hyperpolarization of P cells, produces a positive shift in the P cell GABA reversal potential and enhances P cell synaptic transmission |
| 靶点： |
Potassium Channel |
| 体外研究： |
VU 0240551 reduces the P cell response to GABA in a concentration-dependent manner with 75 and 100 μM treatments causing a significant reduction in GABA-elicited hyperpolarization while 25 μM had no significant effect. |
| 体内研究： |
VU 0240551 (10 μM) significantly blocks the chloride influx in cells from Eu rats but did not affect cells from SL rats. |
| 参考文献： |
1. Delpire E, et al. Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2. Proc Natl Acad Sci U S A. 2009 Mar 31;106(13):5383-8. 2. Wang Y, et al. Differential effects of GABA in modulating nociceptive vs. non-nociceptive synapses. Neuroscience. 2015;298:397-409. 3. Balapattabi K, et al. Effects of salt-loading on supraoptic vasopressin neurones assessed by ClopHensorN chloride imaging. J Neuroendocrinol. 2019;31(8):e12752. |
| 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 |
2.92 ml |
14.601 ml |
29.202 ml |
| 5 mM |
0.584 ml |
2.92 ml |
5.84 ml |
| 10 mM |
0.292 ml |
1.46 ml |
2.92 ml |
| 50 mM |
0.058 ml |
0.292 ml |
0.584 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京