Description | NS19504 is an activator of Ca2+-activated K+ channel with EC50 of 11.0 µM. NS19504 shows relaxing effect on bladder smooth muscle spontaneous phasic contractions[1]. |
In vitro | NS19504在EC50值为11.0 μM时激活BK通道。通过高通量电生理学(QPatch)进行了击中验证,并在表达hBK通道的人类胚胎肾293细胞中通过手动全细胞和内向外膜片钳技术进一步特征描述:NS19504在0.3到10 M的浓度范围内明显激活了BK通道,并使电压激活曲线左移60 mV。此外,全细胞记录显示NS19504在豚鼠尿道平滑肌原生BK通道中引起激活。在豚鼠尿道肌肉条中,1 M浓度的NS19504减少了自发的相位收缩,这种效应被特异性BK通道阻断剂iberiotoxin显著抑制。相比之下,1 M浓度的NS19504只轻微抑制了神经诱导的收缩,并且对高K(+)浓度诱导的收缩没有效果,这与K(+)通道介导的作用一致。 |
Target activity | BK channel:11.0 µM (EC50) |
molecular weight | 269.16 |
Molecular formula | C10H9BrN2S |
CAS | 327062-46-4 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
Solubility | DMSO: 249 mg/mL (925.10 mM), Sonication is recommended. |
References | 1. Nausch B, et al. NS19504: a novel BK channel activator with relaxing effect on bladder smooth muscle spontaneous phasic contractions. J Pharmacol Exp Ther. 2014 Sep;350(3):520-30. |