R-8507 is a small molecule antagonist of the TNF-alpha type 1 receptor (TNF-alphaRI). It inhibits the expression of intercellular adhesion molecule-1 (ICAM-1) induced by TNF-alpha and IL-1beta with EC50 values of 2.45 and 3.79 µM, respectively, in an ELISA using A549 lung epithelial cells. It also disrupts the interaction of the TNF-alphaRI with receptor interacting protein 1 (RIP1) and TNF-alphaR-associated death domain protein (TRADD), preventing internalization of the receptor complex.
