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.
The product specifications provided below refer solely to the active content of MRS2365 trisodium.
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
Description
The product specifications provided below refer solely to the active content of MRS2365 trisodium.
IC50 & Target
[1]|
P2Y1 Receptor 0.4 nM (EC50) |
In Vitro
In Vivo
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 (287 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)