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Submit ReviewMRS 2365
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)
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
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
If you know of a relevant reference for MRS 2365, please let us know.
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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:
Kurahashi et al (2014) Platelet-derived growth factor receptor-α-positive cells and not smooth muscle cells mediate purinergic hyperpolarization in murine colonic muscles. Am J Physiol Cell Physiol 307 C561 PMID: 25055825
Kuboyama et al (2011) Astrocytic P2Y(1) receptor is involved in the regulation of cytokine/chemokine transcription and cerebral damage in a rat model of cerebral ischemia. J Clin Invest 31 1930 PMID: 21487414
Shabir et al (2013) Functional expression of purinergic P2 receptors and transient receptor potential channels by the human urothelium. Neuropsychopharmacology 305 F396 PMID: 23720349
Gao et al (2013) The role of P2Y(14) and other P2Y receptors in degranulation of human LAD2 mast cells. J Cereb Blood Flow Metab 9 31 PMID: 22825617
Chandaka et al (2011) Facilitation of transmitter release from rat sympathetic neurons via presynaptic P2Y(1) receptors. Br J Pharmacol 164 1522 PMID: 21557728
Mamedova et al (2008) Attenuation of apoptosis in vitro and ischemia/reperfusion injury in vivo in mouse skeletal muscle by P2Y6 receptor activation. Purinergic Signal 58 232 PMID: 18805489
Ilatovskaya et al (2013) Pharmacological characterization of the P2 receptors profile in the podocytes of the freshly isolated rat glomeruli. Am J Physiol Cell Physiol 305 C1050 PMID: 24048730
Zhang et al (2019) P2Y1 Purinergic Receptor Modulate Axon Initial Segment Initial Development. Front Cell Neurosci 13 152 PMID: 31068791
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
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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!
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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.