ER-464195-01

ER-464195-01 is a specific, orally active inhibitor that inhibits Calreticulin (CRT) binding to integrin α subunits (ITGAs) with IC50 of 0.17, 0.36, and 0.23 uM in the interaction between CRT and ITGA α4, αL, and αM/α2/α5; dose-dependently and specificly inhibits GST-fused CRT proteins binding to ITGA4 in vitro pull-down assay; inhibits the PMA-induced T cells and the fMLP-stimulated neutrophils bound to VCAM1 (IC50=0.15 μM) and ICAM-1 (IC50=0.19 μM), respectively; suppresses the cell adhesion and the migration of leukocytes, prevents colitis and downregulates the expression of inflammation-related genes in DSS-treated mice, ameliorates the severity of disease in IBD mouse models.

References 1. Ohkuro M, et al. Nat Commun. 2018 May 17;9(1):1982. View Related Products by Target Integrin