Z-3578 

Z-3578 is a small-molecule antagonist targeting MrgX2 (Mas-related G protein-coupled receptor X2) with significant anti-pseudoallergic activity and a K_D value of 729 nM. Z-3578 effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, suppressing the release of β-hexosaminidase with IC₅₀ values of 4.90 µM and 6.18 µM, respectively. It also markedly reduces the release of histamine and TNF-α, 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^[1].

467.37

C₂₃H₁₆Cl₂N₄OS

473687-20-6

O=C(CSC1=NC(C2=CC=CC=C2)=C(N=N1)C3=CC=CC=C3)NC4=C(C=C(C=C4)Cl)Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Xia Z, et al. MrgX2-Targeting Ligand Screen for Antipseudoallergic Agents by Immobilized His-Tag-Fused Protein Technology. J Med Chem. 2025 Mar 13;68(5):5942-5953.  [Content Brief]