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Cangrelor is an ATP analog that inhibits platelet aggregation (IC50 = 0.4 nM).1 It is a reversible competitive antagonist of the platelet purinergic P2Y12 receptor.2,3 Pretreatment with cangrelor significantly reduces blood clotting induced by ADP in a mouse model of pulmonary thromboembolism.4 Formulations containing cangrelor have been used to prevent blood clotting in at-risk patients.5
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1. Antagonists of the platelet P2T receptor: A novel approach to antithrombotic therapy. J. Med. Chem. 42(2), 213-220 (1999).
2. P2Y12 inhibitors: Differences in properties and mechanisms of action and potential consequences for clinical use. Eur. Heart J. 30(16), 1964-1977 (2009).
3. A comparative study of molecular structure, pKa, lipophilicity, solubility, absorption and polar surface area of some antiplatelet drugs. Int. J. Mol. Sci. 17(3), 388 (2016).
4. Quantification of the blood platelet reactivity in the ADP-
5. P2Y12-