Catalog No.: PC-26954Not For Human Use, Lab Use Only.
(Rac)-EVT-401 is the racemate form of EVT-401, a potent, highly selective human P2X7 receptor (P2X7R) antagonist with Ki of 7.6 nM in competitive binding assays.
(Rac)-EVT-401 is the racemate form of EVT-401, a potent, highly selective human P2X7 receptor (P2X7R) antagonist with Ki of 7.6 nM in competitive binding assays.
EVT-401 differentially inhibits P2X7R-mediated calcium influx in 1321N1 cells expressing human and rat P2X7R with IC50 of 10 nM for hP2X7R and 220 nM for rat P2X7R.
EVT-401 does not inhibit the functions of P2X7-related P2 receptors (P2X1R, P2X2R, P2X3R, and P2X4R).
EVT-401 (100 uM) inhibits the proliferation of rheumatoid arthritis synovial fibroblasts (RA SF) by inducing G1 cell cycle arrest.
EVT-401 interferes with the inflammatory phenotypes of RA SF. EVT-401 significantly reduced the clinical arthritis score, diminished swelling in proximal interphalangeal (PIP) joints, and decreased the incidence of PIP arthriti in NHP arthritis.
