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.
For research use only. We do not sell to patients.
- CAS No.: 436847-09-5
- Formula: C13H19N5O9P2S
- Molecular Weight:483.33
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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P2Y1 Receptor 0.4 nM (EC50) |
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 (0.1-2 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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CAS No. 436847-09-5
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Molecular Weight 483.33
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Formula C13H19N5O9P2S
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SMILES
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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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)
MRS2365 Related Classifications
HY-108656 Related Classifications
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