MRS2365 

MRS2365 is a potent and selective P2Y1 receptor (EC₅₀=0.4 nM) /[³⁵S]GTPγS binding/β-arrestin 2 recruitment agonist with an EC₅₀ of 0.4 nM. MRS2365 relieves mechanical allodynia and increases mechanical sensitivity. MRS2365 shows little agonist or antagonist activity at the P2Y12 or P2Y13 receptors^[1][2][3][4].

MRS2365 (1 µM or 3 µM; 2 min) weakens adenosine diphosphate (ADP)-induced platelet aggregation^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MRS2365 (0.03-0.3 mg/kg; i.p.; single dose) significantly alleviates the mechanical allodynia in the male wistar rats neuropathy (Seltzer) model with dose-dependent manner^[3].
MRS2365 (0.1-2 mg/kg; i.p.; single dose) increases the paw withdrawal threshold (PWT) in male wistar rats with neuropathic pain model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

483.33

C₁₃H₁₉N₅O₉P₂S

436847-09-5

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

Room temperature in continental US; may vary elsewhere.

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

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [4]. Gao ZG, et al. Distinct Signaling Patterns of Allosteric Antagonism at the P2Y1 Receptor. Mol Pharmacol. 2017 Nov;92(5):613-626.  [Content Brief]