MRS2578

MRS2578 is a **synthetic small molecule** that acts as a **potent, selective, and insurmountable antagonist of the P2Y6 receptor**, a G protein-coupled purinergic receptor implicated in inflammatory and vascular signaling[1][2][4][7][9][11]. It demonstrates high selectivity for the P2Y6 receptor (IC50 ~37 nM in human), showing minimal or no activity at related P2Y1, P2Y2, P2Y4, and P2Y11 receptors[2][5][9][11][12]. In research contexts, it is used to block P2Y6-mediated responses such as UDP-induced cell signaling, and has been shown to modulate inflammatory cell recruitment, phagocytosis, and cytokine release[1][3][10][13]. Mechanistically, MRS2578 binds to, crosslinks, and oligomerizes the P2Y6 receptor, resulting in effective and irreversible receptor antagonism[6]. MRS2578 is primarily a tool for research use, not approved for clinical therapeutic use[4]. Its effects have been studied in cardiovascular, immunological, and apoptosis-related models, including inhibition of UDP-induced inositol phosphate accumulation and neutrophil extracellular trap (NET) formation[1][10][13].

Other names

1-(3-isothiocyanatophenyl)-3-[4-[(3-isothiocyanatophenyl)carbamothioylamino]butyl]thioureaN,N''-1,4-Butanediylbis[N'-(3-isothiocyanatophenyl)thiourea1,4-Di[3-(3-isothiocyanatophenyl)thioureido]butaneCAS 711019-86-2CAS711019-86-2CAS-711019-86-2