Mas-related G-protein-coupled Receptor (MRGPR) Inhibitor

Z-3578 is an orally active small-molecule antagonist of MrgX2 with potent antipseudoallergic activity, exhibiting a K_D value of 729 nM. Z-3578 effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, suppresses the release of β-hexosaminidase, significantly reduces the release of histamine and TNF-α, and decreases intracellular calcium flux. In a mouse pseudoallergy model, Z-3578 significantly alleviates paw swelling and dye extravasation, and reduces serum histamine levels. Z-3578 can be used for the study of pseudoallergic reactions.

MRGX2-IN-1 is a MRGX2 inhibitor with a pK_d of 7.45 and a pEC₅₀ of 7.867 against hMRGX2. MRGX2-IN-1 can be used for the research of immune diseases.

Catestatin (mouse) is an antimicrobial peptide. Catestatin (mouse) robustly activates Mrgprb2 with an EC₅₀ of 59.73 μM. Catestatin (mouse) is effective in promoting MRSA clearance from wound infections. Catestatin (mouse) dampens the inflammatory immune response to MRSA infection.