MRS 2365

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Cat.No. 2157 - MRS 2365 | C13H16N5O9P2SNa3
Description: Highly potent and selective P2Y1 agonist
Chemical Name: [[(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
Purity: ≥98% (HPLC)
Datasheet
Citations (11)
Reviews
Literature (5)

Biological Activity for MRS 2365

MRS 2365 is a highly potent, selective P2Y1 receptor agonist (EC50 = 0.4 nM). Displays no activity at P2Y12 receptors and only very low agonist activity at P2Y13 receptors (at concentrations up to 1 μM). Increases the upregulation of NTPDase1 by ATPγS.

Licensing Information

Sold under license from the NIH, US Patent 10/169975

Technical Data for MRS 2365

M. Wt 549.28
Formula C13H16N5O9P2SNa3
Storage Store at -20°C
Purity ≥98% (HPLC)
PubChem ID 73755043
InChI Key ZYPJOXVKTCEBCA-PVMCGCOJSA-K
Smiles [Na+].[Na+].[Na+].CSC1=NC(N)=C2N=CN(C3[C@H]4C[C@@]4(COP([O-])(=O)OP([O-])([O-])=O)[C@@H](O)[C@H]3O)C2=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for MRS 2365

Solubility Soluble in water (supplied pre-dissolved at a concentration of 10mM)

Product Datasheets for MRS 2365

Certificate of Analysis / Product Datasheet
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References for MRS 2365

References are publications that support the biological activity of the product.

Ravi et al (2002) Adenine nucleotide analogues locked in a northern methanocarba conformation: enhanced stability and potency as P2Y1 receptor agonists. J.Med.Chem. 45 2090 PMID: 11985476

Chhatriwala et al (2004) 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. 311 1038 PMID: 15345752

Lu et al (2007) Stimulation of the P2Y1 receptor up-regulates nucleoside-triphosphate diphosphohydrolase-1 in human retinal pigment epithelial cells. J.Pharmacol.Exp.Ther. 323 157 PMID: 17626796


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Keywords: MRS 2365, MRS 2365 supplier, potent, selective, P2Y1, agonists, Receptors, Purinergic, purinoceptors, MRS2365, 436847-09-5, P2Y, 2157, Tocris Bioscience

11 Citations for MRS 2365

Citations are publications that use Tocris products. Selected citations for MRS 2365 include:

Koch et al (2015) Impaired cognition after stimulation of P2Y1 receptors in the rat medial prefrontal cortex. J Cereb Blood Flow Metab 40 305 PMID: 25027332

Stefanini et al (2015) RASA3 is a critical inhibitor of RAP1-dependent platelet activation. J Neurosci 125 1419 PMID: 25705885

Filippov et al (2010) The scaffold protein NHERF2 determines the coupling of P2Y1 nucleotide and mGluR5 glutamate receptor to different ion channels in neurons. Pharmacol Res 30 11068 PMID: 20720114

Zhang et al (2019) P2Y1 Purinergic Receptor Modulate Axon Initial Segment Initial Development. Front Cell Neurosci 13 152 PMID: 31068791


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cardiovascular

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P2X and P2Y Receptors

P2X and P2Y Receptors Scientific Review

Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.

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Cardiovascular Poster

Cardiovascular disease remains one of the major causes of morbidity and mortality in the Western world and therefore this therapeutic area continues to be of great interest to researchers. This poster highlights the key GPCRs regulating vascular reactivity.