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Products > GPCR > P2Y Receptor > BPTU (Synonyms: BMS-646786)
Product name : BPTU (Synonyms: BMS-646786)
Item : C2447
Price : 200mg, $950;500mg, $1695; 1g, $2490; 2g, $3590
contact : Send inquiry to: info@acesobio.com
CAS : 870544-59-5
Molecular Weight : 445.43
Formula : C₂₃H₂₂F₃N₃O₃
Storage : at -20°C
Additional information : We offer significant discount for bulky quantity order
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Details:
Description of:BPTU(CAS:870544-59-5)
BPTU IS A P2Y1 antagonist. It has been shown to provide antithrombotic efficacy and reduce bleeding liability.
BPTU blocks the supramaximal fast inhibitory junction potentials (fIJP) in a concentration-dependent manner both in the rat and mouse colon (P<0.0001 for both). The EC50 of BPTU is approximately 0.3 μM and 0.06 μM for the rat and mouse colon, respectively. In the rat colon, addition of the P2Y agonist ADPβS at 10 μM significantly reduces spontaneous contractions to a 43.2±13.4% (N=5) (P=0.0002), and this reduction is blocked by 15 min incubation with BPTU at a concentration of 3 μM (93.3±5.1%). Similar results are obtained in the murine colon where ADPβS at 10 μM reduces the area under the curve (AUC) of contractions to a 15.8±5.1% (N=4) (P<0.0001) and its effect is reversed with BPTU at 3 μM (82.7±3.6%). Addition of MRS2365, a selective P2Y1 agonist, at a concentration of 5 μM significantly reduces spontaneous contractions to a 21.2±4.8% (N=5) (P=0.0002) in the murine colon, and this reduction is blocked by 15 min incubation with BPTU at a concentration of 3 μM (93.1±3.8%). The blockage of the MRS2365-induced response by BPTU at 3 μM also occurs in control conditions (N=5) (10.2±5.5% vs. 86.7±5.0%)

Quality control data:
Quality control by 1H-NMR, 13C-NMR, HPLC and LCMS.
Product will be shipped with supporting analytical data. 

REFERENCES

[1]. Mañé N, et al. BPTU, an allosteric antagonist of P2Y1 receptor, blocks nerve mediated inhibitory neuromuscular responses in the gastrointestinal tract of rodents. Neuropharmacology. 2016 Nov;110(Pt A):376-385.
[2]. Verrijk R, et al. Pharmacokinetics in melanoma-bearing mice of 5-dihydroxyboryl-6-propyl-2-thiouracil (BPTU), a candidate compound for boron neutron capture therapy. Br J Cancer. 1994 Apr;69(4):641-7.

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