TC-I 2014 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。
半岛bd体育手机客户端 描述
TC-I 2014 shows antiallodynic properties in pain models. TC-I 2014 is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 antagonist (IC50: 0.8 nM, 3.0 nM, and 4.4 nM for canine, human and rat channels respectively).
体外活性
TC-I 2014 effectively inhibits cold-induced TRPM8 currents in HEK293 cells stably expressing canine or human TRPM8 (IC50: 0.413 and 1 nM, respectively) [1].
体内活性
TC-I 2014 (10 mg/kg, Orally once) fully avoids icilin-induced WDS [1].
Cas No.
1221349-53-6
分子式
C23H19F6N3O
分子量
467.41
储存和溶解度
DMSO:225.0 mg/mL (481.4 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years