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Home - Products - GPCR/G Protein - Glucagon Receptor - GCGR-IN-17

GCGR-IN-17

CAS No. 1393124-08-7

GCGR-IN-17( PF-06291874 | PF06291874 | PF-6291874 )

Catalog No. M11636 CAS No. 1393124-08-7

A highly potent glucagon receptor antagonist with Ki of 14 nM for hGCGR.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    GCGR-IN-17
  • Note
    Research use only, not for human use.
  • Brief Description
    A highly potent glucagon receptor antagonist with Ki of 14 nM for hGCGR.
  • Description
    A highly potent glucagon receptor antagonist with Ki of 14 nM for hGCGR; shows excellent selectivity against a panel of 69 receptors, ion channels, uptake sites and enzymes; reduces the glucagon-elicited glucose excursion in a dose-dep endent manner in rats; displays low in vivo clearance and excellent oral bioavailability in both rats and dogs.Diabetes Phase 2 Discontinued.
  • In Vitro
    ——
  • In Vivo
    PF-06291874 exposure is approximately dose-proportional with a half-life of ～19.7-22.7 h. PF-06291874 has a fast on and off rate. PF-06291874 is highly bound to human plasma protein, with a mean free fraction of ～0.55%.
  • Synonyms
    PF-06291874 | PF06291874 | PF-6291874
  • Pathway
    GPCR/G Protein
  • Target
    Glucagon Receptor
  • Recptor
    Glucagon Receptor
  • Research Area
    Metabolic Disease
  • Indication
    Diabetes

Chemical Information

  • CAS Number
    1393124-08-7
  • Formula Weight
    503.5134
  • Molecular Formula
    C26H28F3N3O4
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 30 mg/mL
  • SMILES
    O=C(O)CCNC(C1=CC=C([C@@H](OC2=CC(C)=C(C(C)=C2)N3C=C(C=N3)C(F)(F)F)CCC)C=C1)=O
  • Chemical Name
    glucagon receptor antagonists-4, N-[4-[(1S)-1-[3,5-dimethyl-4-[4-(trifluoromethyl)-1H-pyrazol-1-yl]phenoxy]butyl]benzoyl]-

Shipping & Storage Information

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

Reference

1. Guzman-Perez A, et la. Bioorg Med Chem Lett. 2013 May 15;23(10):3051-8.
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