MRS2365 trisodium
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 99.8%
- Formula: C13H16N5Na3O9P2S
- Molecular Weight:549.28
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Storage:
Solution, -20°C, 2 years
Biological Activity
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P2Y1 Receptor 0.4 nM (EC50) |
MRS2365 trisodium (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 trisodium (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.
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Animal Model:Male Wistar rats with neuropathic pain (250-350 g)[3].
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Dosage:0.03, 0.1, 0.3, 1 and 2 mg/kg.
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Administration:Intraperitoneal injection; single dose.
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Result:Relieved mechanical allodynia and increased the paw withdrawal threshold.
Chemical Information
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Appearance Liquid
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Molecular Weight 549.28
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Formula C13H16N5Na3O9P2S
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Color Colorless to light yellow
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Solution, -20°C, 2 years
Purity & Documentation
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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. [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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)