MRS 2365

Cat. No. 2157

MRS 2365 C13H16N5O9P2SNa3 [436847-09-5]

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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

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
Solubility:
Soluble in water (supplied pre-dissolved at a concentration of 10mM)
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
436847-09-5

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Certificate of Analysis / Product Datasheet
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References are publications that support the products' biological activity.

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.

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.

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.

If you know of a relevant reference for MRS 2365 please let us know.

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.

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.

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.

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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Keywords: MRS 2365, supplier, potent, selective, P2Y1, agonists, Receptors, Purinergic, purinoceptors, MRS2365, Tocris Bioscience, Purinergic (P2Y) Receptor Agonist products

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