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Glucagon Receptor

Glucagon receptor antagonists block the receptor through which glucagon raises hepatic glucose output. The glucagon receptor (GCGR) is a class B G protein-coupled receptor (GPCR) expressed mainly in liver and kidney. Expression cloning of the rat receptor in 1993 described its signaling through cyclic adenosine monophosphate (cAMP) and intracellular calcium. Small-molecule antagonists in this list include MK 0893, adomeglivant and PF-06291874, which serve as tools in models of glucose homeostasis and type 2 diabetes. Glucagon (Human, Porcine) is included as the native peptide agonist for receptor activation assays. The set also contains related incretin tools for glucagon-like peptide 1 (GLP-1) research, such as Glucagon-Like Peptide 1 (7-36) Amide and GLP-1R Antagonist 1.

2 Items

  • GRA Ex-25
    Cat. No.
    A20625
    CAS No.
    307983-31-9

    GRA Ex-25

    GRA Ex-25 is an inhibitor of glucagon receptor, with IC50 of 56 and 55 nM for rat and human glucagon receptors, respectively.

    In stock View Details
    1 mg
    $50.00
    2 mg
    $75.00
    All 8 sizes
  • Glucagon receptor antagonist-7
    Cat. No.
    A58103
    CAS No.
    438618-32-7

    Glucagon receptor antagonist-7

    Glucagon receptor antagonist-7 is a potent inhibitor of the human glucagon receptor (hGCGR), demonstrating an IC50 of 181 nM for blocking the binding of 125I-labeled glucagon. With a KDB of 81 nM, it inhibits glucagon-stimulated adenylyl cyclase activity in CHO cells. This compound effectively reduces glucagon-mediated glycogenolysis in human hepatocytes and has been shown to lower blood glucose levels, making it a valuable tool for research in glucose metabolism and diabetes therapeutic strategies.

    In stock View Details
    1 mg
    $380.00
    5 mg
    $1,410.00
    All 2 sizes

2 Items

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