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GPR183 antagonist 33

Chemical Structure : GPR183 antagonist 33

CAS No.: 3054870-33-3

GPR183 antagonist 33

Catalog No.: PC-21880Not For Human Use, Lab Use Only.

GPR183 antagonist 33 is a highly potent, selective GPR183 (Epstein–Barr-virus-induced gene 2, EBI2) antagonist with IC50 of 0.83 nM in cAMP assays, and 1.83 nM in CER-reporter assays.

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    Biological Activity

    GPR183 antagonist 33 is a highly potent, selective GPR183 (Epstein–Barr-virus-induced gene 2, EBI2) antagonist with IC50 of 0.83 nM in cAMP assays, and 1.83 nM in CER-reporter assays.
    GPR183 antagonist 33 strongly reverses 7α,25-OHC-induced cAMP reduction in a dose-dependent manner with an IC50 value of 0.82 nM in HEK293-GPR183 cells.
    GPR183 antagonist 33 shows minor impact on human GPCRome (168 nonolfactory GPCRs, including GPR183) using the PathHunter β-Arrestin assays.
    GPR183 antagonist 33 exhibits strong suppressive activity against GPR183-mediated β-arrestin recruitment with an IC50 value of 0.88 nM.
    GPR183 antagonist 33 displays strong in vitro antimigration and anti-inflammatory activity in monocytes, effectively blocks 7α,25-OHC induced cell migration in a dose-dependent manner with an IC50 value of 0.73 nM.
    GPR183 antagonist 33 (3 mg/kg and 10 mg/kg, oral) effectively improves the pathological symptoms of DSS-induced experimental colitis.

    Physicochemical Properties

    M.Wt 471.37
    Formula C21H19BrN4O2S
    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

    (E)-1-(4-(2-Aminobenzo[d]thiazole-6-carbonyl)piperazin-1-yl)-3-(4-bromophenyl)prop-2-en-1-one

    References

    1. Ruoqing Zeng, et al. J Med Chem. 2024 Feb 28. doi: 10.1021/acs.jmedchem.3c01905.

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