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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Neuronal Signaling>P2 Receptor Antagonists> MRS 2578
	MRS 2578
  • 	MRS 2578

MRS 2578

Price $1
Package 1g
Min. Order: 1g
Supply Ability: 1ton
Update Time: 2020-01-13

Product Details

Product Name: MRS 2578 CAS No.: 711019-86-2
EC-No.: 200-258-5 Min. Order: 1g
Purity: 99% Supply Ability: 1ton
Release date: 2020/01/13
contact: Mary@coreychem.com
Common Name
MRS 2578
CAS Number
711019-86-2
Molecular Weight
472.673
Density
1.3±0.1 g/cm3
Boiling Point
652.7±65.0 °C at 760 mmHg
Molecular Formula
C20H20N6S4
Melting Point
N/A
MSDS
USA
Flash Point
348.5±34.3 °C
Symbol
Article illustrationArticle illustration 
GHS06, GHS08
Signal Word
Danger

 Use of MRS 2578

 
MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors.IC50 value: 37 nM [1]Target: P2Y6 receptorin 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]. 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 [3]. 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].

 Names

Name
1-(3-isothiocyanatophenyl)-3-[4-[(3-isothiocyanatophenyl)carbamothioylamino]butyl]thiourea
Synonym
More Synonyms

 MRS 2578 Biological Activity

Description
MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors.IC50 value: 37 nM [1]Target: P2Y6 receptorin 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]. 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 [3]. 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].
Related Catalog
Signaling Pathways >> GPCR/G Protein >> P2Y Receptor
Research Areas >> Cardiovascular Disease
References

[1]. Mamedova LK, et al. Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors. Biochem Pharmacol, 2004, 67(9), 1763-1770.

[2]. Riegel AK, et al. Selective induction of endothelial P2Y6 nucleotide receptor promotes vascular inflammation. Blood, 2011, 117(8), 2548-2555.

[3]. Vieira RP, et al. Purinergic receptor type 6 contributes to airway inflammation and remodeling in experimental allergic airway inflammation. Am J Respir Crit Care Med, 2011, 184(2), 215-223.

 Chemical & Physical Properties

Density
1.3±0.1 g/cm3
Boiling Point
652.7±65.0 °C at 760 mmHg
Molecular Formula
C20H20N6S4
Molecular Weight
472.673

Company Profile Introduction

Established in 2014,Career Henan Chemical Co. is a manufacturerspecializing in the sale of fine chemicals. Mainly deals in the sales of: Pharmaceutical intermediates OLED intermediates: Pharmaceutical intermediates; OLED intermediates;

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