2387505-47-5

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].

MRS 2279 is a selective, high affinity competitive antagonist of the P2Y1 receptor (Ki = 2.5 nM; IC50 = 51.6 nM). Fails to block nucleotide signaling at most other P2Y receptors (P2Y2, P2Y4, P2Y6, P2Y11 and P2Y12) and potently inhibits ADP-induced aggregation of human blood platelets in vitro (pKB = 8.05).

P2Y1 Receptor: 51.6 nM (IC₅₀)

Desiccate at -20°C

[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. DOI:10.1021/jm990249v
[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. DOI:10.1038/sj.bjp.0704673
[3] Wei W, et al. Mechanical ventilation induces lung and brain injury through ATP production, P2Y1 receptor activation and dopamine release. Bioengineered. 2022 Feb;13(2):2346-2359. DOI:10.1080/21655979.2021.2022269