TC-N 1752 is a potent and orally active inhibitor ofNav1.7, withIC₅₀s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM athNav1.7,hNav1.3,hNav1.4,hNaV1.5andrNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain^[1][2][3].

TC-N 1752 (compound 52) state-dependently inhibits Nav1.7, with IC₅₀of 170 nM on channels that are 20% inactivated and IC₅₀of 3.6 μM on fully noninactivated channels^[1].
TC-N 1752 inhibits hNav1.7, hNav1.8, hNav1.9, rNav1.9, and mNav1.9 with IC₅₀s of 0.2, 0.1, 1.6, 0.5 and 1.4 μM, respectively^[2].

TC-N 1752 (compound 52) (3-30 mg/kg; p.o.) dose-dependently shows analgesic effect in the Formalin model^[1].
TC-N 1752 (3-30 mg/kg; p.o.) decreases thermal hyperalgesia produced by inflammation^[3].
TC-N 1752 (5 mg/mL; 500 μL; i.v.) attenuates complete Freund’s adjuvant (CFA)-induced sensitization of C-fiber nociceptors^[3].

516.52

Solid

C₂₅H₂₇F₃N₆O₃

1211866-85-1

Room temperature in continental US; may vary elsewhere.

DMSO : 125 mg/mL(242.00 mM;Need ultrasonic)

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