MRS 2365

Catalog #: 2157
11 Citations Datasheet / COA / SDS

Catalog #	Availability	Size / Price	Qty
2157/1

1 Image

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%

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Product Details

Citations (11)

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Biological Activity

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.

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

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.

Additional Information

Licensing Caveats:

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

Background References

P2Y1R is involved in visceral hypersensitivity in rats with experimental irritable bowel syndrome
J Wu, Y Cheng, R Zhang, D Liu, YM Luo, KL Chen, S Ren, J Zhang
World J. Gastroenterol., 2017;23(34):6339-6349.
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
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
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
Inhibiting the LPS-induced enhancement of mEPSC frequency in superficial dorsal horn neurons may serve as an electrophysiological model for alleviating pain
CT Yang, SY Hung, SF Hsu, I MacDonald, JG Lin, ST Luo, PL Lin, YH Chen
Sci Rep, 2019;9(1):16032.

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M. Wt* g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Citations for MRS 2365

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

11 Citations: Showing 1 - 10

P2Y1 Purinergic Receptor Modulate Axon Initial Segment Initial Development.
Authors: Zhang Et al.
Front Cell Neurosci 2019;13:152
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
RASA3 is a critical inhibitor of RAP1-dependent platelet activation.
Authors: Stefanini Et al.
J Neurosci 2015;125:1419
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
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
Functional expression of purinergic P2 receptors and transient receptor potential channels by the human urothelium.
Authors: Shabir Et al.
Neuropsychopharmacology 2013;305:F396
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
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
Facilitation of transmitter release from rat sympathetic neurons via presynaptic P2Y(1) receptors.
Authors: Chandaka Et al.
Br J Pharmacol 2011;164:1522
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

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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