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).

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

Medlife 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.

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

Room temperature or refrigerated transportation.

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

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  [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.  [Information]

  [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.  [Information]