1. GPCR/G Protein
  2. P2Y Receptor
  3. MRS2279

MRS2279 

Cat. No.: HY-108657
Handling Instructions

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).

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MRS2279 Chemical Structure

MRS2279 Chemical Structure

CAS No. : 367909-40-8

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Description

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)[1][2].

In Vitro

MRS2279 antagonized 2MeSADP-stimulated inositol phosphate formation in turkey erythrocyte membranes with competitive kinetics (pKB=7.75). High affinity competitive antagonism by MRS2279 was also observed at the human P2Y1 receptor (pKB=8.10) stably expressed in 1321N1 human astrocytoma cells. Antagonism was specific for the P2Y1 receptor since MRS2279 had no effect on activation of the human P2Y2, P2Y4, P2Y6, or P2Y11 receptors by their cognate agonists. MRS2279 also did not block the capacity of ADP to act through the Gi/adenylyl cyclase linked P2Y receptor of platelets to inhibit cyclic AMP accumulation[2].

Molecular Weight

469.71

Formula

C₁₃H₁₈ClN₅O₈P₂

CAS No.

367909-40-8

SMILES

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

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

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Keywords:

MRS2279MRS 2279MRS-2279P2Y ReceptorADPinduceplateletaggregationastrocytomacellspurinergicneurotransmissionInhibitorinhibitorinhibit

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MRS2279
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