MRS2578 is a potent and selective P2Y6 nucleotide receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors.
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MRS 2578 is a selective and potent antagonist of the P2Y6 receptor, demonstrating IC50 values of 37 nM in humans and 98 nM in rats. It shows negligible activity at P2Y1, P2Y2, P2Y4, and P2Y11 receptors[1][2].
体内研究
MRS 2578 (3 mg/kg; i.p.; for 3 days) significantly reduces collagen deposition induced by pressure overload without impacting cardiomyocyte hypertrophy following transverse aortic constriction (TAC)[4].
体外研究
MRS 2578 at 1 μM entirely inhibits the protective effect of UDP against TNFα-induced apoptosis in 1321N1 astrocytoma cells[1].
MRS 2578 at 10 μM completely eliminates TNF-α induced NF-κB reporter activity in HMEC-1 cells. Additionally, MRS 2578 significantly diminishes TNF-α–induced proinflammatory gene expression in these cells at the same concentration[2].
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