Catalog Number: 2157
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.
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.
Additional Information
Licensing Caveats:
Sold under license from the NIH, US Patent 10/169975
Background References
  1. Adenine nucleotide analogues locked in a northern methanocarba conformation: enhanced stability and potency as P2Y1 receptor agonists.
    Ravi et al.
    J.Med.Chem., 2002;45:2090
  2. 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.
    Chhatriwala et al.
    J.Pharmacol.Exp.Ther., 2004;311:1038
  3. Stimulation of the P2Y1 receptor up-regulates nucleoside-triphosphate diphosphohydrolase-1 in human retinal pigment epithelial cells.
    Lu et al.
    J.Pharmacol.Exp.Ther., 2007;323:157
Citations:

The citations listed below are publications that use Tocris products. Selected citations for MRS 2365 include:

9 Citations: Showing 1 - 9
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  1. Impaired cognition after stimulation of P2Y1 receptors in the rat medial prefrontal cortex.
    Authors: Koch Et al.
    J Cereb Blood Flow Metab 2015;40:305
  2. RASA3 is a critical inhibitor of RAP1-dependent platelet activation.
    Authors: Stefanini Et al.
    J Neurosci 2015;125:1419
  3. Platelet-derived growth factor receptor-α-positive cells and not smooth muscle cells mediate purinergic hyperpolarization in murine colonic muscles.
    Authors: Kurahashi Et al.
    Am J Physiol Cell Physiol 2014;307:C561
  4. The role of P2Y(14) and other P2Y receptors in degranulation of human LAD2 mast cells.
    Authors: Gao Et al.
    J Cereb Blood Flow Metab 2013;9:31
  5. Functional expression of purinergic P2 receptors and transient receptor potential channels by the human urothelium.
    Authors: Shabir Et al.
    Neuropsychopharmacology 2013;305:F396
  6. Pharmacological characterization of the P2 receptors profile in the podocytes of the freshly isolated rat glomeruli.
    Authors: Ilatovskaya Et al.
    Am J Physiol Cell Physiol 2013;305:C1050
  7. Astrocytic P2Y(1) receptor is involved in the regulation of cytokine/chemokine transcription and cerebral damage in a rat model of cerebral ischemia.
    Authors: Kuboyama Et al.
    J Clin Invest 2011;31:1930
  8. The scaffold protein NHERF2 determines the coupling of P2Y1 nucleotide and mGluR5 glutamate receptor to different ion channels in neurons.
    Authors: Filippov Et al.
    Pharmacol Res 2010;30:11068
  9. Attenuation of apoptosis in vitro and ischemia/reperfusion injury in vivo in mouse skeletal muscle by P2Y6 receptor activation.
    Authors: Mamedova Et al.
    Purinergic Signal 2008;58:232

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