| Bioactivity | 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[1]. | ||||||||||||
| Target | TRPM8. | ||||||||||||
| Invitro | 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[1]. | ||||||||||||
| In Vivo | TC-I 2014 (10 mg/kg, Orally once) completely prevents icilin-induced WDS[1]. Animal Model: | ||||||||||||
| Name | TC-I 2014 | ||||||||||||
| CAS | 1221349-53-6 | ||||||||||||
| Formula | C23H19F6N3O | ||||||||||||
| Molar Mass | 467.41 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
TC-I 2014
CAS: 1221349-53-6 F: C23H19F6N3O W: 467.41
TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8
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