产品
编 号:F080332
分子式:C23H19F6N3O
分子量:467.41
产品类型
结构图
CAS No: 1221349-53-6
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产品详情
生物活性:
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.
体内研究:
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.
体外研究:
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.