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。
| 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. |
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| 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. |
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| 体内研究 |
TC-I 2014 (10 mg/kg, Orally once) completely prevents icilin-induced WDS.
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| 分子式 |
C23H19F6N3O
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| 分子量 |
467.41
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| CAS号 |
1221349-53-6
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
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