| Identification | Back Directory | [Name]
MRS 2365 | [CAS]
436847-09-5 | [Synonyms]
MRS 2365
MRS 2365, CID: 73755043
Diphosphoric acid, P-[[(1R,2R,3S,4R,5S)-4-[6-amino-2-(methylthio)-9H-purin-9-yl]-2,3-dihydroxybicyclo[3.1.0]hex-1-yl]methyl] ester
[[(1R,2R,3S,4R,5S)-4-[6-Amino-2-(methylthio)-9H-purin-9-yl]-2,3-dihydroxybicyclo[3.1.0]hex-1-yl]methyl]diphosphoricacidmonoestertrisodiumsalt
[[(1R,2R,3S,4R,5S)-4-[6-AMINO-2-(METHYLTHIO)-9H-PURIN-9-YL]-2,3-DIHYDROXYBICYCLO[3.1.0]HEX-1-YL]METHYL] DIPHOSPHORIC ACID MONO ESTER TRISODIUM SALT | [Molecular Formula]
C13H19N5O9P2S | [MDL Number]
MFCD08703094 | [MOL File]
436847-09-5.mol | [Molecular Weight]
483.33 |
| Chemical Properties | Back Directory | [Boiling point ]
875.5±75.0 °C(Predicted) | [density ]
2.37±0.1 g/cm3(Predicted) | [storage temp. ]
Desiccate at -20°C | [form ]
Powder | [pka]
1.42±0.10(Predicted) | [Water Solubility ]
Soluble in water (supplied pre-dissolved at a concentration of 10mM) |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
Highly potent, selective P2Y 1 receptor agonist (EC 50 = 0.4 nM). Displays no activity at P2Y 12 receptors and only very low agonist activity at P2Y 13 receptors (at concentrations up to 1 μ M). | [in vivo]
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].
| Animal Model: | Male Wistar rats with neuropathic pain(250-350 g)[3]. | | Dosage: | 0.03, 0.1, 0.3, 1 and 2 mg/kg. | | Administration: | Intraperitoneal injection; single dose. | | Result: | Relieved mechanical allodynia and increased the paw withdrawal threshold. |
| [IC 50]
P2Y1 Receptor: 0.4 nM (EC50) | [References]
[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. DOI:10.1124/jpet.104.068650
[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. DOI:10.1111/j.1538-7836.2006.01866.x
[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. DOI:10.1111/j.1476-5381.2009.00596.x
[4] Gao ZG, et al. Distinct Signaling Patterns of Allosteric Antagonism at the P2Y1 Receptor. Mol Pharmacol. 2017 Nov;92(5):613-626. DOI:10.1124/mol.117.109660 |
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