MRS 2578

SKU: orb1301012

Description

MRS2578 is a potent and selective P2Y6 receptor antagonist with an IC50 of 37 nM. It is a valuable research tool for investigating the role of uridine nucleotide signaling in inflammatory and immune processes, as demonstrated in various in vitro and in vivo studies.

Research Area

Cell Biology, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 711019-86-2
• MW: 472.67
• Purity: >99.99% (May vary between batches)
• Formula: C₂₀H₂₀N₆S₄
• SMILES: S=C=Nc1cccc(NC(=S)NCCCCNC(=S)Nc2cccc(c2)N=C=S)c1
• Target: P2Y Receptor,Apoptosis
• Solubility: DMSO:23.6 mg/mL (49.93 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.23 mM)

Bioactivity

• Target IC50:
  P2Y6:37 nM
• In Vivo:
  MRS 2578 (10 μM) attenuates Keratinocyte-derived chemokine serum protein levels in LPS-induced vascular inflammation in C57BL/6 mice. MRS2578 (10 μM, intratracheally) reduces BALF eosinophilia and the levels of IL-5 and IL-13 in the BALF in OVA-sensitized mice and leads to a markedly attenuated change in methacholine responsiveness after OVA challenge. MRS2578 (10 μM, intratracheally) inhibits house dust mite–induced allergic airway inflammation in OVA-sensitized mice. MRS2578 (10 μM, intratracheally) reduces of IL-6 and KC levels in BALF in OVA-sensitized mice.
• In Vitro:
  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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, MRS2578, MRS-2578, MRS 2578, inhibit, Inhibitor, P2Y, P2Y Receptor, P2Y6, P2YReceptor

Compound Identifiers

PubChem CID

16078986