GLP-1 Receptors

GLP-1 receptor agonists and modulators act on the receptor for glucagon-like peptide 1 (GLP-1), an incretin hormone. Intestinal L cells release GLP-1 after a meal, and the hormone enhances glucose-dependent insulin secretion from pancreatic beta cells. The receptor, a class B G protein-coupled receptor, was cloned from beta cells by expression cloning in 1992. Peptide agonists in this category include liraglutide and lixisenatide, while tirzepatide also acts at the glucose-dependent insulinotropic polypeptide (GIP) receptor. BETP is a small-molecule ligand that binds the GLP-1 receptor outside the peptide site. The set also includes dipeptidyl peptidase 4 (DPP-4) inhibitors such as linagliptin, which slow the breakdown of endogenous GLP-1.

2 Items

  • WB403
    Cat. No.
    A60398

    WB403

    WB403 is a potent TGR5 activator with an EC50 of 5.5 μM for human TGR5. It enhances downstream signaling pathways associated with glucose metabolism, notably promoting GLP-1 secretion, improving glucose tolerance, and lowering fasting and postprandial blood glucose levels as well as HbA1c in murine models of type 2 diabetes. Additionally, WB403 contributes to increased pancreatic β-cell mass and the restoration of the islet cell distribution. This compound is valuable for studying mechanisms and therapeutic strategies in type 2 diabetes research.

    5 mg
    $80.00
    10 mg
    $130.00
    All 5 sizes
  • 3-Deoxyglucosone
    Cat. No.
    A60597

    3-Deoxyglucosone

    Synonyms: 3-Deoxy-D-glucosone

    3-Deoxyglucosone is a GLP-1 activator that plays a critical role in the Maillard reaction and the polyol pathway. This reactive intermediate interacts with protein amino groups to produce advanced glycation end products (AGEs), particularly imidazolone, the most specific AGE for 3-Deoxyglucosone. Additionally, it enhances GLP-1 secretion in the presence of low glucose levels, positioning it as a valuable biomarker for diabetes research.

    1 mg
    $125.00
    5 mg
    $390.00
    All 2 sizes

2 Items

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