TC-N 1752

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TC-N 1752 是一种有效和具有口服活性的 Nav1.7 抑制剂，抑制 hNav1.7，hNav1.3，hNav1.4，hNaV1.5 和 rNav1.8 的 IC50 值分别为 0.17 μM，0.3 μM，0.4 μM，1.1 μM 和 2.2 μM。TC-N 1752 还抑制河豚毒素敏感的钠通道。TC-N 1752 在福尔马林疼痛模型中显示出镇痛效果。

human NaV1.7 channels blocker.(In Vitro):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. 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).(In Vivo):TC-N 1752 (5 mg/ml; i.v.) attenuates Freund's adjuvant-induced sensitization of C fiber nociceptors. 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.

TC-N 1752 (compound 52) state-dependently inhibits Nav1.7, with IC50 of 170 nM on channels that are 20% inactivated and IC50 of 3.6 μM on fully noninactivated channels.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.

TC-N 1752 (compound 52) (3-30 mg/kg; p.o.) dose-dependently shows analgesic effect in the Formalin model.TC-N 1752 (3-30 mg/kg; p.o.) decreases thermal hyperalgesia produced by inflammation.TC-N 1752 (5 mg/mL; 500 μL; i.v.) attenuates complete Freund’s adjuvant (CFA)-induced sensitization of C-fiber nociceptors. Animal Model:Rats were injected intraplantar with Formalin Dosage:3, 10, 20, 30 mg/kg Administration: Administered p.o. 120 min prior to Formalin Result:Showed analgesic efficacy starting at the dose of 3 mg/kg, with full efficacy at 20 mg/kg dose.

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Others

Other Targets

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1211866-85-1

516.525

C25H27F3N6O3

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (242.00 mM)

C\C(O)=N\c1cccc(\N=c2/ncnc([nH]2)N2CCC(CC2)OCc2ccc(OC(F)(F)F)cc2)c1C

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(-20℃)

With Ice Pack

≥ 2 years