Drug intelligence / Profile preview

BPTU

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Intraperitoneal, Intravenous
01

Overview

BPTU is a synthetic small-molecule non-nucleotide antagonist of the purinergic P2Y1 receptor, originally disclosed by Bristol-Myers Squibb as BMS-646786.[1][5] It binds to an allosteric site located outside the transmembrane helical bundle of the human P2Y1 G protein–coupled receptor, acting as a negative allosteric modulator that inhibits ADP-induced receptor activation, platelet aggregation, and associated thrombotic responses.[4][5][8] In preclinical models, BPTU exhibits antithrombotic activity and blocks P2Y1-mediated neuromuscular inhibitory responses in the gastrointestinal tract, but it is used solely as a pharmacological tool compound for in vitro and in vivo research and has not been developed as a therapeutic drug.[2][4][5]

Other names
1-[2-(2-tert-butylphenoxy)pyridin-3-yl]-3-[4-(trifluoromethoxy)phenyl]ureaN-[2-[2-(1,1-dimethylethyl)phenoxy]-3-pyridinyl]-N'-[4-(trifluoromethoxy)phenyl]urea
02

Targets

P2RY1 (Purinergic Receptor P2Y1)

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