711019-86-2 Usage
Description
MRS 2578 is an antagonist of the purinergic P2Y6 receptor, with high specificity and selectivity for this receptor without affecting other purinergic receptors. It is characterized by its IC50 values of 37 nM for human receptors and 98 nM for rat receptors. MRS 2578 is utilized in various research applications to study the cellular and physiological roles of the P2Y6 receptor.
Uses
Used in Pharmaceutical Research:
MRS 2578 is used as a research tool for studying the role of purinergic P2Y6 receptors in various physiological processes and diseases. It helps researchers understand the receptor's function and its potential as a therapeutic target.
Used in Inflammation Studies:
MRS 2578 is used as an antagonist to investigate the effects of P2Y6 receptors on inflammatory responses. It has been tested in P. aeruginosa infected mice to evaluate its impact on inflammation.
Used in Respiratory Research:
MRS 2578 is used as a selective P2Y6 receptor antagonist in the study of Up4A-induced relaxation in coronary small arteries from swine. This application helps researchers understand the role of purinergic receptors in respiratory health and disease.
Used in Immunology:
MRS 2578 is used as a research compound to test its inhibition on neutrophil extracellular traps and monosodium urate (MSU) crystals formation in polymorphonuclear leukocytes. This application aids in understanding the receptor's role in immune system function and potential therapeutic interventions.
Biological Activity
Selective antagonist of P2Y 6 nucleotide receptors; IC 50 values are 37 and 98 nM at human and rat P2Y 6 receptors respectively. Displays no activity at P2Y 1 , P2Y 2 , P2Y 4 and P2Y 11 receptors (IC 50 > 10 μ M). Inhibits agonist-induced cardiomyocyte contraction and UDP-induced phagocytosis.
Biochem/physiol Actions
MRS 2578 elicits cytoprotective functionality in neuroblastoma cells and prevents dopaminergic neuron death under in vitro and in vivo conditions. It also protects microglia by delaying lipopolysaccharide-induced death.
references
[1] mamedova l k, joshi b v, gao z g, et al. diisothiocyanate derivatives as potent, insurmountable antagonists of p2y6 nucleotide receptors[j]. biochemical pharmacology, 2004, 67(9): 1763-1770.
Check Digit Verification of cas no
The CAS Registry Mumber 711019-86-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 7,1,1,0,1 and 9 respectively; the second part has 2 digits, 8 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 711019-86:
(8*7)+(7*1)+(6*1)+(5*0)+(4*1)+(3*9)+(2*8)+(1*6)=122
122 % 10 = 2
So 711019-86-2 is a valid CAS Registry Number.
711019-86-2Relevant articles and documents
Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors
Mamedova, Liaman K.,Joshi, Bhalchandra V.,Gao, Zhan-Guo,Von Kuegelgen, Ivar,Jacobson, Kenneth A.
, p. 1763 - 1770 (2004)
The physiological role of the P2Y6 nucleotide receptor may involve cardiovascular, immune and digestive functions based on the receptor tissue distribution, and selective antagonists for this receptor are lacking. We have synthesized a series of symmetric aryl diisothiocyanate derivatives and examined their ability to inhibit phospholipase C (PLC) activity induced by activation of five subtypes of recombinant P2Y receptors. Several derivatives were more potent at inhibiting action of UDP at both human and rat P2Y 6 receptors expressed in 1321N1 human astrocytes than activation of human P2Y1, P2Y2, P2Y4 and P2Y11 receptors. The inhibition by diisothiocyanate derivatives of 1,2-diphenylethane (MRS2567) and 1,4-di-(phenylthioureido) butane (MRS2578) was concentration-dependent and insurmountable, with IC50 values of 126±15nM and 37±16nM (human) and 101±27nM and 98±11nM (rat), respectively. A derivative of 1,4-phenylendiisothiocyanate (MRS2575) inhibited only human but not rat P2Y6 receptor activity. MRS2567 and MRS2578 at 10μM did not affect the UTP (100nM)-induced responses of cells expressing P2Y2 and P2Y4 receptors, nor did they affect the 2-methylthio-ADP (30nM)-induced responses at the P2Y1 receptor or the ATP (10μM)-induced responses at the P2Y11 receptor. Other antagonists displayed mixed selectivities. The selective antagonists MRS2567, MRS2575 and MRS2578 (1μM) completely blocked the protection by UDP of cells undergoing TNFα-induced apoptosis. Thus, we have identified potent, insurmountable antagonists of P2Y6 receptors that are selective within the family of PLC-coupled P2Y receptors.
