mPGES1-IN-17d

CAS No. 1469976-70-2

mPGES1-IN-17d( —— )

Catalog No. M12011 CAS No. 1469976-70-2

mPGES1-IN-17d is a potent, selective mPGES-1 inhibitor with enzyme IC50 of 8 nM, A549 cell IC50 of 16.24 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    mPGES1-IN-17d
  • Note
    Research use only, not for human use.
  • Brief Description
    mPGES1-IN-17d is a potent, selective mPGES-1 inhibitor with enzyme IC50 of 8 nM, A549 cell IC50 of 16.24 nM.
  • Description
    mPGES1-IN-17d is a potent, selective mPGES-1 inhibitor with enzyme IC50 of 8 nM, A549 cell IC50 of 16.24 nM, human whole blood IC50 of 249.9 nM; displays excellent in vitro selectivity over mPGES-2, cPGES, COX1/2, other prostanoid synthases, favorable hERG and CEREP panel profile; shows good efficacy in LPS-induced thermal hyperalgesia pain model; demonstrates good oral pharmacokinetic profiles and good CNS B/P ratio in rat and guinea pig.
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Immunology/Inflammation
  • Target
    PGE synthase
  • Recptor
    PGE synthase
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1469976-70-2
  • Formula Weight
    538.859
  • Molecular Formula
    C24H16ClF5N4O3
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    O=C(NC1=CC(F)=CC(C(F)(F)F)=C1)C2=C(OCCO3)C3=C(N(C)C(NC4=C(Cl)C=CC=C4F)=N5)C5=C2
  • Chemical Name
    2-((2-chloro-6-fluorophenyl)amino)-N-(3-fluoro-5-(trifluoromethyl)phenyl)-1-methyl-7,8-dihydro-1H-[1,4]dioxino[2',3':3,4]benzo[1,2-d]imidazole-5-carboxamide

Shipping & Storage Information

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

Reference

1. Muthukaman N, et al. Bioorg Med Chem Lett. 2016 Dec 15;26(24):5977-5984.
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