For research use only.

Catalog No.S4079 Synonyms: AZD 6140, AR-C 126532XX

7 publications

Ticagrelor Chemical Structure

CAS No. 274693-27-5

Ticagrelor (AZD 6140, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM.

Selleck's Ticagrelor has been cited by 7 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.

    Washed platelets were incubated with varying concentrations of ticagrelor using a thrombin EC80. IC50s were calculated.

    J Thromb Haemost, 2018, doi:10.1111/jth.14318. Ticagrelor purchased from Selleck.

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Biological Activity

Description Ticagrelor (AZD 6140, 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.
P2Y12 [1]
2 nM(Ki)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H9c2 MYfGeY5kfGmxbjDhd5NigQ>? M1LmfFAvOSxiMDyzJIFv\CBzIN88US=> NYjh[5Y1OjRiaB?= NWW5SIhK\W[oZXP0bZZmKGmwIILl[JVkcW6pIF7DXFEhemW4ZYLz[UBi[3Srdnn0fUB4cGWwIHzve4VzKGOxbnPlcpRz[XSrb37z MX6zNFczOTdyNB?=
EAhy926 Mm\4RZBweHSxc3nzJIF{e2G7 M3XoZlQxKM7:TTDhcoQhPjBizszN Mo\t[IVkemWjc3Wgc5guVESOLXnu[JVk\WRiYYDvdJRwe2m|LDDwZZJ1cWO3bHHycJkh[XRiYTDobYdp\XJiY3;uZ4VvfHKjdHnvci=> MnzWN|A2QTJ{N{G=
AsPC-1 MV3GeY5kfGmxbjDhd5NigQ>? MnPUNVAh|ryP MmPTNkBp NE\vNFZ1cWOjZ4LlcI9zKG6nZ3H0[YQhfGinIIDsZZRmdGW2IILlcIVie2G2ZTDl[oZm[3Rib36gRYt1NCCHcnugZYN1cX[jdHnvckBidmRiU3z1[{B2eHKnZ4XsZZRqd25? M37nS|I6ODZ2M{i4
BxPC-3 MULGeY5kfGmxbjDhd5NigQ>? MVOxNEDPxE1? MXSyJIg> M3T5S5Rq[2GpcnXsc5IhdmWpYYTl[EB1cGVicHzheIVt\XRicnXs[YF{[XSnIHXm[oVkfCCxbjDBb5QtKEW{azDhZ5RqfmG2aX;uJIFv\CCVbIXnJJVxemWpdXzheIlwdg>? NILPV|czQTB4NEO4PC=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot

PubMed: 27694321     

Representative immunoblots showing VASP-P, VASP, and α-tubulin (internal control) levels in washed platelets after preincubation at 37°C with the following: Ticagrelor (10 µM) for 0, 0.5, 5, 10, 15, 30, and 60 minutes.

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]


Solubility (25°C)

In vitro DMSO 100 mg/mL (191.36 mM)
Water Insoluble
Ethanol '53 mg/mL
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.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 522.57


CAS No. 274693-27-5
Storage powder
in solvent
Synonyms AZD 6140, AR-C 126532XX
Smiles CCCSC1=NC(=C2C(=N1)N(N=N2)C3CC(C(C3O)O)OCCO)NC4CC4C5=CC(=C(C=C5)F)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04976530 Not yet recruiting Device: DrugSorb-ATR system|Device: Sham comparator Hemorrhage Surgical|Blood Loss Surgical|Blood Loss Postoperative|Hemorrhage Postoperative CytoSorbents Inc August 2021 Not Applicable
NCT04739384 Recruiting Drug: Ticagrelor 90mg|Drug: Ticagrelor 60 mg Acute Coronary Syndrome|STEMI|NSTEMI|Coronary Artery Disease|Myocardial Infarction Federico II University|AdvicePharma Group April 1 2021 Phase 3
NCT04471870 Recruiting -- Acute Coronary Syndrome Chiesi Farmaceutici S.p.A. October 23 2020 --

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID