TC-I 2014

Research use only, not for human use.

TC-I 2014 shows antiallodynic properties in pain models.

TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC50 values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively. TC-I 2014 exhibits antiallodynic properties in pain models.

TC-I 2014 (compound 5) potently inhibits cold-induced TRPM8 currents in HEK293 cells stably expressing canine or human TRPM8, with IC50 values of 0.413 and 1 nM, respectively.

TC-I 2014 (10 mg/kg, Orally once) completely prevents icilin-induced WDS.Animal Model:TC-I 2014 (10 mg/kg, Orally once) completely prevents icilin-induced WDS.Dosage:3, 5.6, 10 mg/kg.Administration:Orally once.Result:Produced greater than 90% inhibition at 3, 5.6, and 10 mg/kg administered 2 h prior to icilin challenge.

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Membrane Transporter/Ion Channel

TRP/TRPV Channel

TRP/TRPV Channel

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1221349-53-6

467.41

C23H19F6N3O

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (534.86 mM; Ultrasonic )

FC(F)(F)c1ccccc1-c1cc(c2[nH]c(nc2c1)C1=NOC2(C1)CCCCC2)C(F)(F)F

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(-20℃)

With Ice Pack

≥ 2 years