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Allosteric antagonist of P2Y1 (EC50 = 0.06-0.3 μM). Non-nucleotide ligand. Binds receptor outside of the helical bundle. Blocks inhibition of spontaneous contraction of rat and mouse colon induced by electrical field stimulation, nicotine and P2Y agonists. Antithrombotic; reduces platelet aggregation.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 445.43. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.25 mL||11.23 mL||22.45 mL|
|5 mM||0.45 mL||2.25 mL||4.49 mL|
|10 mM||0.22 mL||1.12 mL||2.25 mL|
|50 mM||0.04 mL||0.22 mL||0.45 mL|
References are publications that support the biological activity of the product.
Chao et al (2013) Discovery of 2-(phenoxypyridine)-3-phenylureas as small molecule P2Y1 antagonists. J.Med.Chem. 2013 1704 PMID: 23368907
Zhang et al (2015) Two disparate ligand-binding sites in the human P2Y1 receptor. Nature. 2015 317 PMID: 25822790
Mañé et al (2016) BPTU, an allosteric antagonist of P2Y1 receptor, blocks nerve mediated inhibitory neuromuscular responses in the gastrointestinal tract of rodents. Neuropharmacology. 2016 376 PMID: 27496690
If you know of a relevant reference for BPTU, please let us know.
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Keywords: BPTU, BPTU supplier, P2Y1, antagonists, antagonism, antithrombotic, non-nucleotide, ligand, spontaneous, contraction, allosteric, NAM, Purinergic, P2Y, Receptors, 6078, Tocris Bioscience
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