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MRS2365 (trisodium)

MRS2365 trisodium is a potent and selective P2Y1 receptor (EC50=0.4 nM) /[35S]GTPγS binding/β-arrestin 2 recruitment agonist. MRS2365 trisodium relieves mechanical allodynia and increases mechanical sensitivity[1][2][3][4].

Product Specifications

UNSPSC

12352005

Target

Arrestin; P2Y Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/mrs2365-trisodium.html

Concentration

10 mM * 182 μL in Water

Purity

99.0

Solubility

10 mM in DMSO

Smiles

O=P(OP(O[Na])(O[Na])=O)(O[Na])OC[C@]12[C@@H](O)[C@@H](O)[C@H](N3C=NC4=C(N)N=C(SC)N=C34)[C@@]1([H])C2

Molecular Formula

C13H16N5Na3O9P2S

Molecular Weight

549.28

References & Citations

[1]Mariya Chhatriwala, et al. Induction of novel agonist selectivity for the ADP-activated P2Y1 receptor versus the ADP-activated P2Y12 and P2Y13 receptors by conformational constraint of an ADP analog. J Pharmacol Exp Ther. 2004 Dec;311 (3) :1038-43.|[2]D M Bourdon, et al. (N) -methanocarba-2MeSADP (MRS2365) is a subtype-specific agonist that induces rapid desensitization of the P2Y1 receptor of human platelets. J Thromb Haemost. 2006 Apr;4 (4) :861-8.|[3]Andó RD, et al. A comparative analysis of the activity of ligands acting at P2X and P2Y receptor subtypes in models of neuropathic, acute and inflammatory pain. Br J Pharmacol. 2010 Mar;159 (5) :1106-17. |[4]Gao ZG, et al. Distinct Signaling Patterns of Allosteric Antagonism at the P2Y1 Receptor. Mol Pharmacol. 2017 Nov;92 (5) :613-626.

Shipping Conditions

Blue Ice

Storage Conditions

Solution, -20°C, 2 years

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

P2Y1 Receptor

Curated Selection

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