MRS2279
Based on 1 publication(s) in Google Scholar
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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- CAS. Nr.: 367909-40-8
- Formel: C13H18ClN5O8P2
- Molecular Weight:469.71
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) MRS2279
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Biologische Aktivität
Beschreibung
IC50 & Target
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P2Y1 Receptor 51.6 nM (IC50) |
In Vitro
MRS2279 antagonizes 2-MeSADP-stimulated inositol phosphate formation in turkey erythrocyte membranes with a pKb value of 7.75[2]. MRS2279 shows high affinity competitive antagonism to human P2Y1 receptor with a pKb 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. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 367909-40-8
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Molecular Weight 469.71
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Formel C13H18ClN5O8P2
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SMILES
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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Bioengineered
Mechanical ventilation induces lung and brain injury through ATP production, P2Y1 receptor activation and dopamine release. [Abstract]2022 Feb;13(2):2346-2359. PMID: 35034579
Reinheit & Dokumentation
Verweise
[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]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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