Catalog No.S4079 Synonyms: AZD 6140
Molecular Weight(MW): 522.57
Ticagrelor is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM.
Cited by 5 Publications
2 Customer Reviews
Effect of antiplatelet drugs on platelet aggregation in healthy individuals. Samples from healthy individuals were preincubated with anti-platelet drugs (n = 3). Curves and columns show mean platelet aggregation and the relationship between platelet aggregation and drug concen-tration. Bars represent standard deviations. *P < 0.05 as compared with platelet aggregation with the same agonist but no drugs added; pairedStudent’s t-test. (A-C) The drugs tested were abciximab (A), ticagrelor (B), and vorapaxar (C).
J Thromb Haemost, 2017, 15(6):1191-1202. Ticagrelor purchased from Selleck.
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Choose Selective P2 Receptor Inhibitors
|Description||Ticagrelor is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM.|
|Features||First-in-class of a new type of P2Y12 antagonist known as cyclopentyl-triazolo-pyrimidines.|
Ticagrelor is an active drug which, does not require metabolic activation after intestinal absorption. It does not compete directly with ADP at the ADP binding site but occupies an adjacent binding site and acts in an allosteric way, resulting in a reversible conformational change of the receptor. Ticagrelor binds reversibly to the receptor and exhibits rapid onset and offset of effect. Binding studies in rh-P2Y12 receptor-transfected CHO-K1 cells indicate that ticagrelor exhibits potent, rapid, and reversible binding, with a Kd of 10.5 nM, a kon (association constant) of 0.00011/(nM•s), a koff (dissociation constant) of 0.00087/s, and half-life values of 4 min for binding and 14 min for unbinding, indicating that the magnitude of platelet inhibition is dependent on concentrations of drug available to bind platelets.  Ticagrelor moderately inhibits CYP2C9 activity in human liver microsomes, while exhibiting little or no inhibition of CYP1A2, CYP2B6, CYP2C8, CYP2C19, CYP2D6, and CYP2E1. In human liver microsomes, ticagrelor inhibits midazolam 4-hydroxylation, while activating 1_-hydroxylation of midazolam. Evaluated in fresh human hepatocytes, ticagrelor is not an inducer of CYP1A2 or CYP3A4. 
|In vivo||Absorption of ticagrelor is rapid with t max of 1.3-2 h. And the Cmax and area under the plasma concentration-time curve from time 0 to infinity increases in an apparently dose-proportional manner over the dose range studied, indicating linear pharmacokinetics. The mean terminal-phase half-life (t1/2) is approximately 7-8.5 h for ticagrelor. Inhibition of platelet aggregation (IPA) is dose related and is nearly complete at 2 h at doses of 100-400 mg. Ticagrelor is well tolerated, with no serious or doserelated adverse events or notable changes in laboratory values observed. |
|In vitro||DMSO||100 mg/mL (191.36 mM)|
|Ethanol||53 mg/mL (101.42 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04088123||Not yet recruiting||Drug: Ticagrelor Oral Tablet [Brilinta]||Thrombosis; Artery||George Washington University|National Institute on Minority Health and Health Disparities (NIMHD)|Shenandoah University|GWU Medical Faculty Associates||October 2019||--|
|NCT02302508||Withdrawn||Drug: Clopidogrel Prasugrel Ticagrelor||Diabetes||Centre hospitalier de l''Université de Montréal (CHUM)|Centre de Recherche du Centre Hospitalier de l''Université de Montréal||September 1 2019||Phase 4|
|NCT03658005||Not yet recruiting||Other: Blood sample||Acute Coronary Syndrome||Centre Hospitalier Universitaire de Besancon||September 1 2018||--|
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