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Mapracorat

CAS No. 887375-26-0

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

Catalog No. M16416 CAS No. 887375-26-0

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

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Mapracorat
  • Note
    Research use only, not for human use.
  • Brief Description
    Mapracorat (ZK 245186) is a potent, selective and non-steroid glucocorticoid receptor (GR) agonist with binding Ki of 1.9 nM.
  • Description
    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.
  • In Vitro
    Mapracorat concentration dependently inhibited TNFα secretion from activated canine PBMC with IC50 value of approximately 0.2 nM.
  • In Vivo
    Intradermal injection of compound 48/80 (50 μg in 50 μL saline) resulted in a clear wheal and flare reaction over the 60 min observation period. Topical pre-treatment with mapracorat (0.1%) leads to significant reduction in the wheal and flare responses compared to vehicle (acetone) treated areas.
  • Synonyms
    ZK 245186 | BOL 303242X | BAY-865319
  • Pathway
    Endocrinology/Hormones
  • Target
    GR
  • Recptor
    GR
  • Research Area
    Inflammation/Immunology
  • Indication
    Psoriasis

Chemical Information

  • CAS Number
    887375-26-0
  • Formula Weight
    462.489
  • Molecular Formula
    C25H26F4N2O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : ≥ 33.6 mg/mL 72.65 mM
  • SMILES
    CC(C)(C1=CC(F)=CC2=C1OCC2)C[C@@](O)(CNC3=C4C=CC(C)=NC4=CC=C3)C(F)(F)F
  • Chemical Name
    (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

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Sch?cke 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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