Description: AMG 517 is an effective and specific TRPV1 antagonist, antagonizes proton (IC50: 0.76 nM), capsaicin (IC50: 0.62 nM), and heat activation (IC50: 1.3 nM) of TRPV1. Target: TRP/TRPV Channel. Smiles: O(C1=C2C(SC(NC(C)=O)=N2)=CC=C1)C=3C=C(N=CN3)C4=CC=C(C(F)(F)F)C=C4. References: Gavva NR, et al. J Pharmacol...

AMG 517 is an antagonist of transient receptor potential vanilloid 1 (TRPV1, IC50 = 0.9 nM). It inhibits mechanical and thermal allodynia in a rat model of burn injury when administered intrathecally at a dose of 165 µg. AMG 517 (150 and 300 µg/kg) also reverses increases in the level of calcitonin gene-related...