MR S2578

Description	MRS2578 selectively blocks P2Y6 receptor activity versus activity at P2Y1, P2Y2, P2Y4 or P2Y11 receptors. MRS2578 (1 μM) completely blocks the protection by UDP undergoing TNFalpha-induced apoptosis in 1321N1 astrocytoma cells.MRS 2578 inhibits basal NF-κB activity in time and dose dependent manner in HMEC-1 cells transfected with 0.25 μg NF-κB promoter reporter. MRS 2578 (10 μM) completely abolishes TNF-α induced NF-κB reporter activity in HMEC-1 cells. MRS 2578 (10 μM) significant reduces TNF-α–induced proinflammatory gene expression in HMEC-1 cells. MRS 2578 potentiates ATPγS and UDP response at concentrations below 316 nM whereas above this concentration, MRS 2578 inhibits ATPS- and UDP-induced IP accumulation in neonatal rat cardiac myofibroblasts.MRS2578-treated mice shows reduced bronchial hyperresponsiveness toward methacholine in OVA-sensitized mice. MRS2578 completely blocks UDP-induced the release of IL-6, KC, and IL-8 in lung epithelial cells.
Pathways	Ion Channel/Membrane Transporter Neuro Signaling Pathway GPCR/G Protein
Targets	P2 Receptor

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