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Mapracorat

Chemical Structure : Mapracorat

CAS No.: 887375-26-0

Mapracorat (ZK 245186;BOL 303242X;BAY-865319)

Catalog No.: PC-61603Not For Human Use, Lab Use Only.

Mapracorat (ZK 245186) is a potent, selective and non-steroid glucocorticoid receptor (GR) agonist with binding Ki of 1.9 nM.

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    Biological Activity

    Mapracorat (ZK 245186) is a potent, selective and non-steroid glucocorticoid receptor (GR) agonist with binding Ki of 1.9 nM; does not show significant activity for ERα, PR, AR or MR; shows anti-inflammatory efficacy after topical application similar to the classical glucocorticoids, with a better safety profile.

    Psoriasis

    Phase 1 Clinical

    Physicochemical Properties

    M.Wt 462.489
    Formula C25H26F4N2O2
    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

    (2R)-1,1,1-trifluoro-4-(5-fluoro-2,3-dihydro-1-benzofuran-7-yl)-4-methyl-2-[[(2-methylquinolin-5-yl)amino]methyl]pentan-2-ol

    References

    1. Schäcke H, et al. Br J Pharmacol. 2009 Oct;158(4):1088-103.

    2. Zhang JZ, et al. Mol Vis. 2009 Dec 8;15:2606-16.

    3. Shafiee A, et al. Invest Ophthalmol Vis Sci. 2011 Mar 14;52(3):1422-30.

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