BPTU

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Cat.No. 6078 - BPTU | C23H22F3N3O3 | CAS No. 870544-59-5
Description: P2Y1 allosteric antagonist
Chemical Name: N-[2-[2-(1,1-Dimethylethyl)phenoxy]-3-pyridinyl]-N'-[4-(trifluoromethoxy)phenyl]urea
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 44.54 100
ethanol 44.54 100

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 solvent 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

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: BPTU, supplier, P2Y1, antagonists, antagonism, antithrombotic, non-nucleotide, ligand, spontaneous, contraction, allosteric, Purinergic, P2Y, Receptors, Purinergic, P2Y, Receptors, Tocris Bioscience

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