MRS 2365

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Cat.No. 2157 - MRS 2365 | C13H16N5O9P2SNa3 | CAS No. 436847-09-5
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 (9)
Literature

Biological Activity

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

M. Wt 549.28
Formula C13H16N5O9P2SNa3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 436847-09-5
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 549.28. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.82 mL 9.1 mL 18.21 mL
5 mM 0.36 mL 1.82 mL 3.64 mL
10 mM 0.18 mL 0.91 mL 1.82 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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: potent selective P2Y1 agonists Receptors Purinergic purinoceptors MRS2365 Purinergic P2Y Receptors

9 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

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

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

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

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

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

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


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