Name: Ticagrelor
Brand: Selleck Chemicals
SKU: S4079
Availability: InStock
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Quality Control

Batch: Purity: 99.88%

99.88

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE)
Other P2 Receptor Inhibitors	A-438079 Hydrochloride A-804598 MRS 2578 A-740003 5-BDBD JNJ-47965567 BX430 Eliapixant Aurintricarboxylic acid A-317491

Cell Culture, Treatment & Working Concentration

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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (191.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	6.700mg/ml (12.82mM)	Taking the 1 mL working solution as an example, add 50 μL of 134 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

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%

Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight	522.57	Formula	C₂₃H₂₈F₂N₆O₄S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	274693-27-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	AZD6140, AR-C 126532XX			Smiles	CCCSC1=NC(=C2C(=N1)N(N=N2)C3CC(C(C3O)O)OCCO)NC4CC4C5=CC(=C(C=C5)F)F

Mechanism of Action

Features	First-in-class of a new type of P2Y12 antagonist known as cyclopentyl-triazolo-pyrimidines.
Targets/IC₅₀/Ki	P2Y12 2 nM(Ki)
In vitro	Ticicagrelor 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. This compound 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 this compound exhibits potent, rapid, and reversible binding, with a K_d of 10.5 nM, a k_on (association constant) of 0.00011/(nM•s), a k_off (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. This chemical 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, it inhibits midazolam 4-hydroxylation, while activating 1_-hydroxylation of midazolam. Evaluated in fresh human hepatocytes, this compound is not an inducer of CYP1A2 or CYP3A4.
Kinase Assay	Binding assays using P2Y12-transfected CHO-K1 or humanplatelet membranes
Kinase Assay	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.
In vivo	Absorption of ticagrelor is rapid with t _max of 1.3-2 h. And the C_max 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 (t_1/2) is approximately 7-8.5 h for this compound. Inhibition of platelet aggregation (IPA) is dose related and is nearly complete at 2 h at doses of 100-400 mg. This chemical is well tolerated, with no serious or doserelated adverse events or notable changes in laboratory values observed.
References	[1] https://pubmed.ncbi.nlm.nih.gov/19552634/ [2] https://pubmed.ncbi.nlm.nih.gov/20091161/ [3] https://pubmed.ncbi.nlm.nih.gov/21177984/ [4] https://pubmed.ncbi.nlm.nih.gov/32523112/

Applications

Methods	Biomarkers	Images	PMID
Western blot	VASP-P / VASP		27694321

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Ticagrelor P2 Receptor antagonist

Chemical Structure

Molecular Weight: 522.57