An allosteric P2Y1 receptor antagonist (Ki = 6 nM for the human receptor); selective for P2Y1 over P2Y2

BPTU – 5 mg

Brand:
Cayman
CAS:
870544-59-5
Storage:
-20
UN-No:
Non-Hazardous - /

BPTU is an allosteric antagonist of the purinergic P2Y1 receptor (Ki = 6 nM for the human receptor).{53133,53134} BPTU is selective for P2Y1 over P2Y2, P2Y6, P2Y11, P2Y12, and P2Y14 receptors (Kis = ≥3,500 nM).{53133} 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).{53134}  

 

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Description

An allosteric P2Y1 receptor antagonist (Ki = 6 nM for the human receptor); selective for P2Y1 over P2Y2, P2Y6, P2Y11, P2Y12, and P2Y14 receptors with (Kis = ≥3,500 nM); inhibits platelet aggregation in hPRP (IC50 = 2.1 µM); 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 at a 10 mg/kg bolus dose followed by a 10 mg/kg per hour infusion; 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

Synonyms: 

Molecular weight: 445.4

CAS: 870544-59-5

Purity: ≥98%

Formulation: A solid

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