MRS2279 diammonium 是一种选择性、高亲和力的 P2Y1 受体拮抗剂，K_i 为 2.5 nM，IC₅₀ 为 51.6 nM。MRS2279 diammonium 竞争性抑制 ADP 促进的血小板聚集，pK_b 值为 8.05。

MRS2279 diammonium is a selective and high affinity P2Y1 receptor antagonist, with a K i value of 2.5 nM and an IC 50 value of 51.6 nM. MRS2279 diammonium competitively inhibits ADP-promoted platelet aggregation with an pK b value of 8.05.

Solid

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.
MRS2279 diammonium shows high affinity competitive antagonism to human P2Y1 receptor with a pKb value of 8.10 in 1321N1 human astrocytoma cells.
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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Nandanan E, et al. Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y(1) receptor ligands. J Med Chem. 2000;43(5):829-842.
[2]. Boyer JL, et al, Ravi RG, Jacobson KA, Harden TK. 2-Chloro N(6)-methyl-(N)-methanocarba-2-deoxyadenosine-3,5-bisphosphate is a selective high affinity P2Y(1) receptor antagonist. Br J Pharmacol. 2002;135(8):2004-2010.