TC-N 1752 是一种具有口服活性的 Nav1.7 通道抑制剂，IC50 为 0.17 μM。 TC-N 1752 显示镇痛活性。

TC-N 1752 is an orally active inhibitor of Nav1.7 channel with IC50 of 0.17 μM. TC-N 1752 shows analgesic activities.

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].

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].

1211866-85-1

C25H27F3N6O3

516.52

DMSO:112.5mg/mL (217.8mM),Need ultrasonic
1eq. HCl:<5.17mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years