TC-N 1752

TC-N 1752CAS号: 1211866-85-1分子式: C25H27F3N6O3分子量: 516.52描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
TC-N 1752 is an orally active inhibitor of Nav1.7 channel with IC50 of 0.17 μM. TC-N 1752 shows analgesic activities.
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:112.5mg/mL (217.8mM)
生物活性
靶点
hNa v 1.7:0.17 μM (IC50), hNa v 1.3:0.3 μM (IC50), hNa v 1.4:0.4 μM (IC50), hNa v 1.5:1.1 μM (IC50), hNa v 1.8:0.1 μM (IC50)
In vitro(体外研究)
TC-N 1752 exhibits IC50s of 0.2, 0.1, 1.6, 0.5 and 1.4 μM for hNav1.7, hNav1.8, hNav1.9, rNav1.9, and mNav1.9[1]. TC-N 1752 state-dependently inhibits Nav1.7 channel on channels that are 20% inactivated(IC50 = 170 nM) and on fully noninactivated channels(IC50 = 3.6 μM)[1].
In vivo(体内研究)
TC-N 1752 (5 mg/ml; i.v.) attenuates Freund’s adjuvant-induced sensitization of C fiber nociceptors[2]. TC-N 1752 (3-30 mg/kg; orally) exhibits analgesic effects in a dose-dependent manner in a formalin model and reduces thermal hyperalgesia produced by inflammation[3].