备注 |
AMG 517 is a potent and selective TRPV1 antagonist, antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM. |
生化机理 |
The vanilloid receptor TRPV1 has been identified as a molecular target for the treatment of pain associated with inflammatory diseases and cancer. AMG 517 is a potent and selective transient receptor potential vanilloid-1 (TRPV1) antagonist. AMG 517 was selected as a second-generation candidate for further evaluation in human clinical trials as a potential new treatment for chronic pain. |
别名 |
Acetamide, N-[4-[[6-[4-(trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]-;Acetamide, N-[4-[[6-[4-(trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]- |