Home Neuronal Signaling P2 Receptor inhibitor MRS 2578

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MRS 2578 P2 Receptor inhibitor

Cat.No.S2855

MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, and exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors.
MRS 2578 P2 Receptor inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 472.67

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Quality Control

Batch: S285501 DMSO]42 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.02%
99.02

Chemical Information, Storage & Stability

Molecular Weight 472.67 Formula

C20H20N6S4

 Storage (From the date of receipt)
CAS No. 711019-86-2 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=CC(=CC(=C1)N=C=S)NC(=S)NCCCCNC(=S)NC2=CC(=CC=C2)N=C=S

Solubility

In vitro
Batch:

DMSO : 42 mg/mL (88.85 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
P2Y6 [1]
37 nM
In vitro
MRS2578 selectively blocks P2Y6 receptor activity versus activity at P2Y1, P2Y2, P2Y4 or P2Y11 receptors. This compound (1 μM) completely blocks the protection by UDP undergoing TNFalpha-induced apoptosis in 1321N1 astrocytoma cells. [1] It inhibits basal NF-κB activity in time and dose dependent manner in HMEC-1 cells transfected with 0.25 μg NF-κB promoter reporter. This chemical (10 μM) completely abolishes TNF-α induced NF-κB reporter activity in HMEC-1 cells. It (10 μM) significant reduces TNF-α–induced proinflammatory gene expression in HMEC-1 cells. [2] The compound potentiates ATPγS and UDP response at concentrations below 316 nM whereas above this concentration, it 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. This compound 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] This compound (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. This compound (10 μM, intratracheally) inhibits house dust mite–induced allergic airway inflammation in OVA-sensitized mice. This compound (10 μM, intratracheally) reduces of IL-6 and KC levels in BALF in OVA-sensitized mice. [4]
References

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