BPTU

BPTU is an allosteric antagonist of the purinergic P2Y1 receptor (Ki = 6 nM for the human receptor). BPTU is selective for P2Y1 over P2Y2, P2Y6, P2Y11, P2Y12, and P2Y14 receptors (Kis = >3,500 nM). It inhibits platelet aggregation in human platelet-rich plasma (hPRP, IC50 = 2.1 µM). BPTU reduces thrombus weight by 68% in a rat model of iron chloride-induced arterial thrombosis and prolongs provoked cuticle and mesenteric bleeding time in rats when administered intravenously as a 10 mg/kg bolus dose followed by a 10 mg/kg per hour infusion. It also inhibits contractions induced by electrical field stimulation in isolated muscle strips from rat and mouse colon (EC50s = 0.5 and 0.1 µM, respectively) and antrum (EC50s = 9 and 0.3 µM, respectively).Formal Name: N-[2-[2-(1,1-dimethylethyl)phenoxy]-3-pyridinyl]-N'-[4-(trifluoromethoxy)phenyl]-urea. CAS Number: 870544-59-5. Molecular Formula: C23H22F3N3O3. Formula Weight: 445.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 15mg/mL, DMSO: 25mg/mL, DMSO:PBS (pH 7.2) (1:2): 0.3mg/mL, Ethanol: 15mg/mL. lambdamax: 260, 288 nm. SMILES: CC(C)(C)C1=CC=CC=C1OC2=C(NC(NC3=CC=C(OC(F)(F)F)C=C3)=O)C=CC=N2. InChi Code: InChI=1S/C23H22F3N3O3/c1-22(2,3)17-7-4-5-9-19(17)31-20-18(8-6-14-27-20)29-21(30)28-15-10-12-16(13-11-15)32-23(24,25)26/h4-14H,1-3H3,(H2,28,29,30). InChi Key: AHFLGPTXSIRAQK-UHFFFAOYSA-N.