MRS 2578 [711019-86-2]
Cat# T6172-25mg
Size : 25mg
Brand : TargetMol
MRS 2578
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COA LCMS HNMR
MRS 2578
Catalog No. T6172Cas No. 711019-86-2
MRS2578, an effective P2Y6 receptor antagonist with IC50 of 37 nM, shows insignificant inhibition at P2Y1, P2Y2, P2Y4, and P2Y11 receptors.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. Pack Size | |
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5 mg | |
10 mg | |
25 mg | |
50 mg | |
100 mg | |
200 mg | |
1 mL x 10 mM (in DMSO) |
Product Introduction
Bioactivity
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. |
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) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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Keywords
inhibitApoptosisP2Y ReceptorMRS-2578MRS2578MRS 2578Inhibitor