BPTU

SKU: orb1303115

Description

BPTU (BMS-646786) is a potent, non-nucleotide allosteric P2Y1 receptor antagonist (EC50 0.06-0.3 µM) that binds outside the helical bundle. It has demonstrated antithrombotic effects by inhibiting platelet aggregation and has been used in vitro and in vivo to study colon motility and purinergic signaling.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 870544-59-5
• MW: 445.43
• Purity: 99.37%
• Formula: C₂₃H₂₂F₃N₃O₃
• SMILES: CC(C)(C)c1ccccc1Oc1ncccc1NC(=O)Nc1ccc(OC(F)(F)F)cc1
• Target: P2Y Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.49 mM);DMSO:35.71 mg/mL (80.17 mM)

Bioactivity

• Target IC50:
  P2Y1:0.06-0.3 μM(EC50)
• In Vivo:
  Octreotide-treated groups show a significant reduction in the tumor volume when compared with saline group. Octreotide-PPSG (1.4 mg/kg, i.p.) shows greater antitumor effect than Octreotide-soln (100 μg/kg, i.p.). Octreotide-treatments results in significant inhibitory effect on the expression levels of SSTR2 and SSTR5 in primary HCC-bearing rats compared with the saline group. Octreotide-PPSG appears to inhibit the expression of SSTR2 and SSTR5 to a greater extent than that of Octreotide-soln treated group. A test dose of octreotide acetate significantly decreases the serum gastrin level to approximately one third of the baseline in 2 hr and the effect lasted approximately for 6 hr. On day 21, treatment with sustained-release formulation of octreotide acetatea (5 mg intramuscular, q 4 wk) is initiated.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

thrombosis, inhibit, P2YReceptor, P2Y1, P2Y Receptor, P2Y, Inhibitor, antithrombotic, BPTU, BMS646786, BMS-646786, BMS 646786

Compound Identifiers

PubChem CID

11510579