MRS2279 diammonium

MRS2279 diammonium is a selective and high affinity P2Y1 receptor antagonist, with a Ki value of 2.5 nM and an IC50 value of 51.6 nM. MRS2279 diammonium competitively inhibits ADP-promoted platelet aggregation with an pKb value of 8.05[1][2][3].

Signaling Pathways >> GPCR/G Protein >> P2Y Receptor

Research Areas >> Neurological Disease

P2Y1 Receptor:51.6 nM (IC50)

MRS2279 diammonium antagonizes 2-MeSADP-stimulated inositol phosphate formation in turkey erythrocyte membranes with a pKb value of 7.75[2]. MRS2279 diammonium shows high affinity competitive antagonism to human P2Y1 receptor with a pKb value of 8.10 in 1321N1 human astrocytoma cells[2]. MRS2279 diammonium shows specific effect for the P2Y1 receptor, but shows no effect on activation of the human P2Y2, P2Y4, P2Y6, or P2Y11 receptors by their cognate agonists[2]. MRS2279 diammonium shows no ability to block the capacity of ADP to act through the Gi/adenylyl cyclase linked P2Y receptor of platelets to inhibit cyclic AMP accumulation[2].

MRS2279 diammonium (2 μL, 1 nM; intracerebroventricular injection; 30 min prior to mechanical ventilation) reduces mouse brain injury induced by mechanical ventilation in high-pressure ventilation mice[3].