TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC 50 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.
性状
Solid
IC50 & Target[1][2]
TRPM8.
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
TC-I 2014 (10 mg/kg, Orally once) completely prevents icilin-induced WDS. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: TC-I 2014 (10 mg/kg, Orally once) completely prevents icilin-
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Parks DJ, et Design and optimization of benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonists. J Med Chem. 2011 Jan 13;54(1):233-47.
溶解度数据
In Vitro: DMSO : 250 mg/mL (534.86 mM; Need ultrasonic)配制储备液