ER-464195-01

ER-464195-01 is an orally active calreticulin (CRT) and integrin α subunits (ITGAs) binding inhibitor. ER-464195-01 inhibits leukocyte infiltration and subsequent inflammatory cascade reactions by dissociating the binding between CRT and ITGA. ER-464195-01 down-regulates the expression of pro-inflammatory genes (such as TNF-α, IL-1β, IL-6, IL-17f) induced by DSS (HY-116282C), and inhibit the phosphorylation of STAT3 and the production of serum amyloid A (SAA). ER-464195-01 can be used for the study of inflammatory bowel disease (IBD)^[1]. In Vitro:ER-464195-01 (5 μM) effectively inhibits the interaction between CRT and ITGA4 within the Jurkat cells and significantly reduces the level of CRT on the cell surface^[1].
ER-464195-01 (0.01-10 μM, 60 min) inhibits the adhesion ability of VCAM-1 cells stimulated by PMA (HY-18739) and ICAM-1 cells stimulated by fMLP (HY-P0224), with IC₅₀ values of 0.15 μM and 0.19 μM respectively, and has no inhibitory effect under MnCl₂ stimulation^[1].
In Vivo:ER-464195-01 (5-10 mg/kg, p.o., once daily for 6-32 days) ameliorates the severity of diseases in IBD mouse models through both prophylactic and therapeutic administration^[1].