Home Neuronal Signaling P2 Receptor antagonist Ticagrelor For research use only.

Ticagrelor

Synonyms: AZD6140, AR-C 126532XX

Ticagrelor (AZD6140, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM.

Ticagrelor Chemical Structure

Ticagrelor Chemical Structure

CAS No. 274693-27-5

Purity & Quality Control

Ticagrelor Related Products

Signaling Pathway

P2 Receptor Signaling Pathways

P2 Receptor Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H9c2 Function assay 0.1, 0,3 and 1 μM 24 h effective in reducing NCX1 reverse activity when lower concentrations 30721704
EAhy926 Apoptosis assay 40 μM and 60 μM decrease ox-LDL-induced apoptosis, particularly at a higher concentration 30592271
AsPC-1 Function assay 10 μM 2 h ticagrelor negated the platelet releasate effect on Akt, Erk activation and Slug upregulation 29064388
BxPC-3 Function assay 10 μM 2 h ticagrelor negated the platelet releasate effect on Akt, Erk activation and Slug upregulation 29064388
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Biological Activity

Description Ticagrelor (AZD6140, AR-C 126532XX) 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.
Targets
P2Y12 [1]
2 nM(Ki)
In vitro
In vitro

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. [1]

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. [3]
Kinase Assay Binding assays using P2Y12-transfected CHO-K1 or humanplatelet membranes
Membranes (5 μg of protein) are added to a 96-well plate containing [125I]AZ11931285 (125 pM), [3H]ADP (10 nM), or [33P]2MeS-ADP (62.5 pM), the required concentration of competitor, and a sufficient volume of buffer (50 mM Tris, 5 mM MgCl2, 50 mM NaCl, and 0.1% nucleotide-free BSA, pH 7.4) to bring the total volume in each well to 200 μL. Binding studies using platelet membranes and [3H]ADP are performed in the presence of 100 μM (final concentration) MRS2179 to prohibit binding to P2Y1. The signal-to-noise ratios for P2Y12-transfected CHO-K1 cells are approximately 14 for [3H]ADP (specific signal: 895 c.p.m.), 24 for [33P]2MeSADP (specific signal: 3308 c.p.m.), and 24 for [125I]AZ11931285 (specific signal: 3308 c.p.m.). For the studies using platelet membranes, the signal-to-noise ratios are approximately 2 for [33P]2MeS-ADP and [3H]ADP and 1.5 for [125I]AZ11931285, with a specific signal between 100 and 400 c.p.m. In this study, an incubation time of 1 h at 30 癈 is used to allow full equilibrium to be achieved. Thereafter, free radioligand is separated from bound radioligand and counted as described above.
Cell Research Cell lines BMDMs
Concentrations 20 μM
Incubation Time 30 minutes
Method

Cells were treated with indicated concentration of drug for 30 minutes.
Experimental Result Images Methods Biomarkers Images PMID
Western blot VASP-P / VASP 27694321
In Vivo
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. [2]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05774431 Recruiting
Acute Myocardial Infarction
University Hospital Heidelberg|AstraZeneca
 March 13 2023 --
NCT05283356 Recruiting
Severe Aortic Valve Stenosis|Aortic Valve Stenosis|Transcatheter Aortic Valve Replacement (TAVR)|Transcatheter Aortic Valve Implantation (TAVI)
Fundacin Biomedica Galicia Sur
 January 21 2022 Phase 4

Chemical Information & Solubility

Molecular Weight 522.57 Formula

C23H28F2N6O4S
CAS No. 274693-27-5 SDF Download Ticagrelor SDF
Smiles CCCSC1=NC(=C2C(=N1)N(N=N2)C3CC(C(C3O)O)OCCO)NC4CC4C5=CC(=C(C=C5)F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (191.36 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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