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BPTU

Chemical Structure : BPTU

CAS No.: 870544-59-5

BPTU (BMS-646786, BMS646786)

Catalog No.: PC-61413Not For Human Use, Lab Use Only.

BPTU (BMS-646786) is a potent, highly selective and allosteric antagonist of P2Y1 receptor with Ki of 6 nM for hP2Y1.

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Biological Activity

BPTU (BMS-646786) is a potent, highly selective and allosteric antagonist of P2Y1 receptor with Ki of 6 nM for hP2Y1.
BPTU shows no significant affinity for hP2Y2/6/11/12/14 (Ki>5 uM).
BPTU inhibits purinergic inhibitory junction potentials and inhibition of spontaneous motility induced by electrical field stimulation in the colon of rats (EC50 = 0.3 uM) and mice (EC50 = 0.06 uM).
BPTU also blocks nicotine induced relaxation, has reasonable plasma exposure, clearance and half-life with moderate oral bioavailability.

Physicochemical Properties

M.Wt 445.43
Formula C23H22F3N3O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[2-[2-(1,1-Dimethylethyl)phenoxy]-3-pyridinyl]-N'-[4-(trifluoromethoxy)phenyl]urea

References

1. Chao H, et al. J Med Chem. 2013 Feb 28;56(4):1704-14.

2. Mañé N, et al. Neuropharmacology. 2016 Nov;110(Pt A):376-385.

3. Zhang D, et al. Nature. 2015 Apr 16;520(7547):317-21.

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