MRS2279 

MRS2279 is a selective and high affinity P2Y1 receptor antagonist, with a K_i of 2.5 nM and an IC₅₀ of 51.6 nM. MRS2279 competitively inhibits ADP-promoted platelet aggregation with an apparent affnity (pK_B=8.05)^[1][2][3].

MRS2279 antagonizes 2-MeSADP-stimulated inositol phosphate formation in turkey erythrocyte membranes with a pK_b value of 7.75^[2].
MRS2279 shows high affinity competitive antagonism to human P2Y1 receptor with a pK_b value of 8.10 in 1321N1 human astrocytoma cells^[2].
MRS2279 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 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MRS2279 (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

469.71

C₁₃H₁₈ClN₅O₈P₂

367909-40-8

O=[P](O)(O)OC[C@]1([C@H]2O[P](O)(O)=O)[C@]([C@](N3C4=NC(Cl)=NC(NC)=C4N=C3)([H])C2)([H])C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]