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编 号:F601002
分子式:C13H18ClN5O8P2
分子量:469.71
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生物活性:
MRS2279 is a selective and high affinity P2Y1 receptor antagonist, with a Ki of 2.5 nM and an IC50 of 51.6 nM. MRS2279 competitively inhibits ADP-promoted platelet aggregation with an apparent affnity (pKB=8.05).

体内研究:
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.

体外研究:
MRS2279 antagonizes 2-MeSADP-stimulated inositol phosphate formation in turkey erythrocyte membranes with a pKb value of 7.75.MRS2279 shows high affinity competitive antagonism to human P2Y1 receptor with a pKb 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.
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