Ticagrelor

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

For research use only.

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

Ticagrelor Chemical Structure

CAS No. 274693-27-5

Selleck's Ticagrelor has been cited by 8 Publications

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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.
Targets
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 M1jKUmZ2dmO2aX;uJIF{e2G7 Mk\GNE4yNCByLEOgZY5lKDFizszN MXuyOEBp NUPCZo1U\W[oZXP0bZZmKGmwIILl[JVkcW6pIF7DXFEhemW4ZYLz[UBi[3Srdnn0fUB4cGWwIHzve4VzKGOxbnPlcpRz[XSrb37z M{L6fVMxPzJzN{C0
EAhy926 MnTXRZBweHSxc3nzJIF{e2G7 MV60NEDPxE1iYX7kJFYxKM7:TR?= NXT1cJAy\GWlcnXhd4Uhd3hvTFTMMYlv\HWlZXSgZZBweHSxc3nzMEBx[XK2aXP1cIFzdHliYYSgZUBpcWeqZYKgZ49v[2WwdILheIlwdg>? MnPRN|A2QTJ{N{G=
AsPC-1 NFHYcJhHfW6ldHnvckBie3OjeR?= MYexNEDPxE1? Mm\yNkBp MnLzeIlk[We{ZXzvdkBv\WejdHXkJJRp\SCybHH0[YxmfCC{ZXzlZZNifGViZX\m[YN1KG:wIFHreEwhTXKtIHHjeIl3[XSrb36gZY5lKFOudXegeZBz\We3bHH0bY9v M{\wSVI6ODZ2M{i4
BxPC-3 NXj4dHBNTnWwY4Tpc44h[XO|YYm= NVfnNpNKOTBizszN NF2zVXozKGh? NWLIN|ExfGmlYXfy[YxweiCwZXfheIVlKHSqZTDwcIF1\WyndDDy[Yxm[XOjdHWg[YZn\WO2IH;uJGFsfCxiRYLrJIFkfGm4YYTpc44h[W6mIGPseYchfXC{ZXf1cIF1cW:w M4T0dFI6ODZ2M{i4
Assay
Methods Test Index PMID
Western blot VASP-P / VASP 27694321
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]

Protocol (from reference)

Solubility (25°C)

In vitro

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.

10mg/mL

Chemical Information

Molecular Weight 522.57
Formula

C23H28F2N6O4S

CAS No. 274693-27-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCSC1=NC(=C2C(=N1)N(N=N2)C3CC(C(C3O)O)OCCO)NC4CC4C5=CC(=C(C=C5)F)F

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05053828 Enrolling by invitation Drug: Antiplatelet Drug Type2 Diabetes|Antiplatelet Drugs|Myocardial Infarction|Heart Failure Tabula Rasa HealthCare September 20 2021 --
NCT04976530 Recruiting Device: DrugSorb-ATR system|Device: Sham comparator Hemorrhage Surgical|Blood Loss Surgical|Blood Loss Postoperative|Hemorrhage Postoperative CytoSorbents Inc August 31 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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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