MRS 2578

Names

[ Name ]:
MRS 2578

[Synonym ]:
1,1'-(1,4-Butanediyl)bis[3-(3-isothiocyanatophenyl)(thiourea)]
Thiourea, N,N''-1,4-butanediylbis[N'-(3-isothiocyanatophenyl)-
MRS 2578
MRS2578

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.

[Related Small Molecules]

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

[ Flash Point ]:
348.5±34.3 °C

[ Exact Mass ]:
472.063232

[ PSA ]:
201.20000

[ LogP ]:
5.10

[ Vapour Pressure ]:
0.0±2.0 mmHg at 25°C

[ Index of Refraction ]:
1.687

[ Storage condition ]:
2-8°C

[ Water Solubility ]:
DMSO: ~17 mg/mL

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS06, GHS08

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301-H312 + H332-H315-H319-H334-H335

[ Precautionary Statements ]:
P261-P284-P301 + P310 + P330-P302 + P352 + P312-P304 + P340 + P312-P342 + P311

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ Hazard Codes ]:
Xn

[ Risk Phrases ]:
20/21/22-36/37/38-42

[ Safety Phrases ]:
22-26-36/37/39-45

[ RIDADR ]:
UN 2811

[ WGK Germany ]:
3

Articles

Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors.

Biochem. Pharmacol. 67 , 1763-1770, (2004)

The physiological role of the P2Y(6) nucleotide receptor may involve cardiovascular, immune and digestive functions based on the receptor tissue distribution, and selective antagonists for this recept...

Activated microglia cause reversible apoptosis of pheochromocytoma cells, inducing their cell death by phagocytosis.

J. Cell Sci. 129 , 65-79, (2016)

Some apoptotic processes, such as phosphatidylserine exposure, are potentially reversible and do not necessarily lead to cell death. However, phosphatidylserine exposure can induce phagocytosis of a c...