TC-I 2014

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-I 2014 hydrochloride 是一种口服有效的、强效的、苯并咪唑类的、 TRPM8 的拮抗剂，其对犬类、人和大鼠通道的IC50 值分别为 0.8 nM, 3.0 nM 和 4.4 nM。在疼痛动物模型中具有抗痛觉超敏作用。

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 中的溶解度 : 250 mg/mL (534.86 mM; 超声助溶 )

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