AMG 517

AMG 517 is a potent and selective small molecule antagonist of the Transient Receptor Potential Vanilloid 1 (TRPV1) receptor, originally developed by Amgen for the treatment of chronic and inflammatory pain. TRPV1 is a non-selective cation channel involved in the detection of noxious heat and pain signaling. While AMG 517 demonstrated high potency in preclinical models, its clinical development was discontinued after Phase 1 and Phase 2 trials revealed that it caused significant and sustained hyperthermia (fever) in human subjects. This side effect is attributed to the role of TRPV1 in thermoregulation. Despite its failure as a therapeutic, AMG 517 remains a widely used pharmacological tool in laboratory research to investigate TRPV1-mediated pathways in various tissues, including airway smooth muscle and sensory neurons.

Other names

N-(4-(6-(4-(trifluoromethyl)phenyl)pyrimidin-4-yloxy)benzothiazol-2-yl)acetamide