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MK-0893

CAS No. 870823-12-4

MK-0893( MK0893 | MK 0893 )

Catalog No. M16326 CAS No. 870823-12-4

A potent, selective, reversible and competitive antagonist of glucagon receptor with high binding affinity (IC(=50=6.6 nM) and functional cAMP activity (IC50=15.7 nM).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    MK-0893
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, selective, reversible and competitive antagonist of glucagon receptor with high binding affinity (IC(=50=6.6 nM) and functional cAMP activity (IC50=15.7 nM).
  • Description
    A potent, selective, reversible and competitive antagonist of glucagon receptor with high binding affinity (IC(=50=6.6 nM) and functional cAMP activity (IC50=15.7 nM); displays selectivity for glucagon receptor relative to other family B GPCRs, IC50 of 1020 nM for GIPR, 9200 nM for PAC1, and >10000 nM for GLP-1R, VPAC1, and VPAC2; blunts glucagon-induced glucose elevation in hGCGR mice and rhesus monkeys, also lowers ambient glucose levels in both acute and chronic mouse models.Diabetes Phase 2 Discontinued.
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    MK0893 | MK 0893
  • Pathway
    GPCR/G Protein
  • Target
    Glucagon Receptor
  • Recptor
    Glucagon Receptor
  • Research Area
    Metabolic Disease
  • Indication
    Diabetes

Chemical Information

  • CAS Number
    870823-12-4
  • Formula Weight
    588.4805
  • Molecular Formula
    C32H27Cl2N3O4
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    CC(C1=CC=C(C=C1)C(=O)NCCC(=O)O)N2C(=CC(=N2)C3=CC(=CC(=C3)Cl)Cl)C4=CC5=C(C=C4)C=C(C=C5)OC
  • Chemical Name
    .beta.-Alanine, N-[4-[(1S)-1-[3-(3,5-dichlorophenyl)-5-(6-methoxy-2-naphthalenyl)-1H-pyrazol-1-yl]ethyl]benzoyl]-

Shipping & Storage Information

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

Reference

1. Xiong Y, et al. J Med Chem. 2012 Jul 12;55(13):6137-48. 2. Guan HP, et al. J Lipid Res. 2015 Nov;56(11):2183-95. 3. Jazayeri A, et al. Nature. 2016 May 12;533(7602):274-7.
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