Z-3578

Description

Z-3578 is a small-molecule antagonist targeting MrgX2 Mas-related G protein-coupled receptor X2 with significant anti-pseudoallergic activity and a KD value of 729 nM. Z-3578 effectively inhibits mast cell degranulation induced by substance P SP and C48/80, suppressing the release of ?-hexosaminidase with IC50 values of 4.90 AAasAasAAmuM and 6.18 AAasAasAAmuM, respectively. It also markedly reduces the release of histamine and TNF-?, along with intracellular calcium flux. In a murine pseudoallergy model, Z-3578 significantly alleviates paw swelling and dye extravasation and lowers serum histamine levels, indicating potent in vivo anti-allergic effects. Z-3578 holds promise as a lead compound for the treatment of allergic diseases, especially pseudoallergic reactions.