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Description: P2Y1 allosteric antagonist
Chemical Name: N-[2-[2-(1,1-Dimethylethyl)phenoxy]-3-pyridinyl]-N'-[4-(trifluoromethoxy)phenyl]urea
Purity: ≥98% (HPLC)
Biological Activity for BPTU
BPTU is an 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.
Technical Data for BPTU
| M. Wt | 445.43 |
| Formula | C23H22F3N3O3 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 870544-59-5 |
| PubChem ID | 11510579 |
| InChI Key | AHFLGPTXSIRAQK-UHFFFAOYSA-N |
| Smiles | CC(C)(C1=C(C=CC=C1)OC2=C(C=CC=N2)NC(NC3=CC=C(C=C3)OC(F)(F)F)=O)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.
Solubility Data for BPTU
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 44.54 | 100 | |
| ethanol | 44.54 | 100 |
Preparing Stock Solutions for BPTU
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 |
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Product Datasheets for BPTU
References for BPTU
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
Citations for BPTU
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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P2X and P2Y Receptors Scientific Review
Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.