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CR6086

Chemical Structure : CR6086

CAS No.: 2502965-92-4

CR6086 (Vorbipiprant, CR-6086)

Catalog No.: PC-20854Not For Human Use, Lab Use Only.

CR6086 (Vorbipiprant) is a potent, selective prostaglandin E2 receptor 4 (EP4) antagonist with Ki of 16.6 nM (hEP4 receptor), inhibits PGE2-stimulated cAMP production with IC50 of 22 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    CR6086 (Vorbipiprant) is a potent, selective prostaglandin E2 receptor 4 (EP4) antagonist with Ki of 16.6 nM (hEP4 receptor), inhibits PGE2-stimulated cAMP production with IC50 of 22 nM.
    CR6086 reduces key cytokine players of RA (IL-6 and VEGF expression in macrophages, IL-23 release from dendritic cells, IL-17 release from Th17 cells) in models of human immune cells in culture.
    CR6086 significantly improves all features of arthritis: severity, histology, inflammation and pain in CIA models of RA in rats and mice.
    CR6086 is better than the selective COX-2 inhibitor rofecoxib and at least as effective as the JAK inhibitor tofacitinib.

    Physicochemical Properties

    M.Wt 472.51
    Formula C26H27F3N2O3
    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

    (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl)benzoic acid

    References

    1. Caselli G, et al. Arthritis Res Ther. 2018 Mar 1;20(1):39.

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