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ER-464195-01

Chemical Structure : ER-464195-01

CAS No.: 859218-37-4

ER-464195-01 (ER464195-01)

Catalog No.: PC-35072Not For Human Use, Lab Use Only.

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.

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    Biological Activity

    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.
    ER-464195-01 dose-dependently and specificly inhibits GST-fused CRT proteins binding to ITGA4 in vitro pull-down assay.
    ER-464195-01 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.
    ER-464195-01 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.

    Physicochemical Properties

    M.Wt 379.029
    Formula C23H39ClN2
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    1-propyl-4-(2-(3,3,5,5-tetramethylcyclohexyl)phenyl)piperazine hydrochloride

    References

    1. Ohkuro M, et al. Nat Commun. 2018 May 17;9(1):1982.

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