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MRS 2578

Catalog No. T6172   CAS 711019-86-2

MRS2578, an effective P2Y6 receptor antagonist with IC50 of 37 nM, shows insignificant inhibition at P2Y1, P2Y2, P2Y4, and P2Y11 receptors.

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MRS 2578 Chemical Structure
MRS 2578, CAS 711019-86-2
Pack Size Availability Price/USD Quantity
5 mg In stock $ 38.00
10 mg In stock $ 48.00
25 mg In stock $ 105.00
50 mg In stock $ 178.00
100 mg In stock $ 287.00
200 mg In stock $ 432.00
1 mL * 10 mM (in DMSO) In stock $ 41.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description MRS2578, an effective P2Y6 receptor antagonist with IC50 of 37 nM, shows insignificant inhibition at P2Y1, P2Y2, P2Y4, and P2Y11 receptors.
Targets&IC50 P2Y6:37 nM
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. [1] 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. [2] 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. [3] 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. [4]
In vivo MRS 2578 (10 μM) attenuates Keratinocyte-derived chemokine serum protein levels in LPS-induced vascular inflammation in C57BL/6 mice. [2] 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. [4]
Molecular Weight 472.67
Formula C20H20N6S4
CAS No. 711019-86-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 23.6 mg/mL (50 mM)

TargetMolReferences and Literature

1. Mamedova LK, et al. Biochem Pharmacol, 2004, 67(9), 1763-1770. 2. Riegel AK, et al. Blood, 2011, 117(8), 2548-2555. 3. Talasila A, et al. Br J Pharmacol, 2009, 158(1), 339-353. 4. Vieira RP, et al. Am J Respir Crit Care Med, 2011, 184(2), 215-223.

Related compound libraries

This product is contained In the following compound libraries:
Neuronal Signaling Compound Library Apoptosis Compound Library NO PAINS Compound Library Inhibitor Library Covalent Inhibitor Library Bioactive Compounds Library Max Target-Focused Phenotypic Screening Library Bioactive Compound Library GPCR Compound Library

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Keywords

MRS 2578 711019-86-2 Apoptosis GPCR/G Protein Neuroscience P2Y Receptor inhibit MRS-2578 MRS2578 Inhibitor inhibitor

 

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