MRGPR

MRGPR ligands act on Mas-related G protein-coupled receptors found on sensory neurons and mast cells. Mas-related G protein-coupled receptors (MRGPRs) were described in 2001 as a large family expressed in subsets of nociceptive sensory neurons. In 2009, mouse Mrgprs were shown to act as itch receptors that mediate chloroquine-induced pruritus. A 2015 study linked the mast cell receptor Mrgprb2, the mouse ortholog of human Mas-related G protein-coupled receptor X2 (MRGPRX2), to pseudo-allergic drug reactions. Most compounds here act on MRGPRX2, including the antagonists Z-3578 and BER-5 and the agonist PAMP-12 (unmodified). ML382 acts on the related receptor Mas-related G protein-coupled receptor X1 (MRGPRX1) as a positive allosteric modulator. BAM(8-22), a bovine adrenal medulla peptide fragment, also activates MRGPRX1.

5 Items

  • Z-3578
    Cat. No.
    A26231

    Z-3578

    Z-3578 is an orally active small-molecule antagonist of the MrgX2 receptor, demonstrating potent antipseudoallergic effects with a KD value of 729 nM. This compound effectively inhibits mast cell degranulation triggered by substances such as substance P and C48/80, leading to reduced release of β-hexosaminidase, histamine, and TNF-α, while also decreasing intracellular calcium flux. In murine models of pseudoallergy, Z-3578 has been shown to significantly diminish paw swelling, dye extravasation, and serum histamine levels, making it suitable for research into pseudoallergic reactions.

    5 mg
    $130.00
    10 mg
    $220.00
    All 5 sizes
  • BER-5
    Cat. No.
    A36050

    BER-5

    BER-5 is a potent antagonist of the MrgX2 receptor, effectively inhibiting a wide variety of MrgX2 agonists. This compound demonstrates the ability to prevent Substance P-induced degranulation in LAD2 mast cells and reduces Substance P-triggered allergic reactions in murine models. BER-5 is suitable for research applications focused on the mechanisms underlying allergic responses.

    Out of stock

    All 3 sizes
  • Mrgx2 antagonist-3
    Cat. No.
    A61577

    Mrgx2 antagonist-3

    MrgX2 antagonist-3 is a highly selective antagonist of the MrgX2 receptor, exhibiting an IC50 value between 0.042 and 2.5 nM. This compound effectively inhibits downstream G protein signaling and β-Arrestin recruitment, which results in the blockade of MrgX2 receptor-mediated calcium influx and cellular degranulation. MrgX2 antagonist-3 serves as a valuable tool in the investigation of inflammation-related diseases and pruritic conditions, including chronic urticaria and allergic asthma.

    5 mg
    $295.00
    10 mg
    $485.00
    All 5 sizes
  • Mrgx2 antagonist-2
    Cat. No.
    A61581

    Mrgx2 antagonist-2

    Mrgx2 antagonist-2 is a selective antagonist of the MrgX2 receptor, exhibiting a pIC50 of 8.6. This compound serves as a valuable tool in the investigation of MrgX2-mediated physiological and pathological processes. It has potential applications in research related to various diseases and disorders associated with the MrgX2 receptor.

    5 mg
    $400.00
    10 mg
    $655.00
    All 5 sizes
  • Mrgx2 antagonist-1
    Cat. No.
    A61586

    Mrgx2 antagonist-1

    Mrgx2 antagonist-1 is a potent antagonist of the Mas-related Gene X2 (MrgX2) receptor. This compound is utilized in research focused on disorders associated with MrgX2 signaling, providing insights into its role in various pathophysiological conditions. The distinct mechanism of action makes Mrgx2 antagonist-1 a valuable tool in studying the therapeutic potential of targeting MrgX2 in relevant disease models.

    25 mg
    $1,800.00
    50 mg
    $2,285.00
    All 3 sizes

5 Items

Added to your cart

View Cart Checkout

    Loading...