Cayman BPTU

BPTU is an allosteric antagonist of the purinergic P2Y₁ receptor (K_i = 6 nM for the human receptor).^, BPTU is selective for P2Y₁ over P2Y₂, P2Y₆, P2Y₁₁, P2Y₁₂, and P2Y₁₄ receptors (K_is = ≥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).

WARNING This product is not for human or veterinary use.