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Ticagrelor

Name: Ticagrelor
Brand: TargetMol
SKU: T0179
Price: 40 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T0179Cas No. 274693-27-5

Alias AZD6140, AR-C 126532XX

Ticagrelor (AR-C 126532XX), produced by AstraZeneca, is an inhibitor of platelet aggregation. Unlike clopidogrel, ticagrelor is not a prodrug required metabolic activation. The drug was approved for use in the European Union by the European Commission on December 3, 2010, and by the US FDA on July 20, 2011. Its trade names are Brilinta (US), Brilique(EU) and Possia(EU).

Ticagrelor

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Purity: 99.77%

Catalog No. T0179Alias AZD6140, AR-C 126532XXCas No. 274693-27-5

Pack Size	Price	USA Warehouse	Global Warehouse
10 mg	$40	In Stock	In Stock
25 mg	$60	In Stock	In Stock
50 mg	$73	In Stock	In Stock
100 mg	$90	In Stock	In Stock
500 mg	$129	-	In Stock
1 g	$197	-	In Stock
1 mL x 10 mM (in DMSO)	$53	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.77%

Color:White

Resource Download

COA HNMR HPLC

Product Introduction

Bioactivity

Description	Ticagrelor (AR-C 126532XX), produced by AstraZeneca, is an inhibitor of platelet aggregation. Unlike clopidogrel, ticagrelor is not a prodrug required metabolic activation. The drug was approved for use in the European Union by the European Commission on December 3, 2010, and by the US FDA on July 20, 2011. Its trade names are Brilinta (US), Brilique(EU) and Possia(EU).
Targets&IC50	P2Y12:2 nM(Ki)
In vitro	Ticagrelor has a half-life (t1/2) of approximately 7-8.5 hours and exhibits a dose-related inhibition of platelet aggregation; a 100-400 mg dose achieves complete inhibition within 2 hours. It is well-tolerated, with no serious adverse events or significant changes in laboratory values observed. Ticagrelor is rapidly absorbed, reaching peak levels in 1.3-2 hours. Within the studied dosage range, both the peak concentration of Ticagrelor and the area under the curve (from time zero to infinity) increase in a dose-proportional manner, indicating linear pharmacokinetics.
In vivo	In binding studies on CHO-K1 cells transfected with rh-P2Y12 receptors, Ticagrelor exhibited efficient and reversible binding, with a kon (association rate constant) of 0.00011/(nM·s), a Kd (equilibrium dissociation constant) of 10.5 nM, and a koff (dissociation rate constant) of 0.00087/s. The half-lives for association and dissociation were 4 and 14 minutes, respectively, suggesting that the concentration of the drug that binds to platelets determines the extent of platelet inhibition. Ticagrelor is an active drug that does not require metabolic activation. It does not directly compete with ADP at the ADP binding site but rather occupies a nearby site, causing a change in the conformation of the binding site that leads to a reversible conformational change in the receptor. The binding of Ticagrelor to the receptor is reversible with quick onset/off rates.
Synonyms	AZD6140, AR-C 126532XX

Chemical Properties

Molecular Weight	522.57
Formula	C₂₃H₂₈F₂N₆O₄S
Cas No.	274693-27-5
Smiles	CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(F)c(F)c2)c2nnn([C@@H]3C[C@H](OCCO)[C@@H](O)[C@H]3O)c2n1
Relative Density.	1.67

Storage & Solubility Information

Storage

keep away from moisture | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (478.4 mM), Sonication is recommended.

In Vivo Formulation

5% DMSO+40 % PEG300+5 % Tween 80+50 % Saline: 5 mg/mL (9.57 mM), Solution.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9136 mL	9.5681 mL	19.1362 mL	95.6810 mL
5 mM	0.3827 mL	1.9136 mL	3.8272 mL	19.1362 mL
10 mM	0.1914 mL	0.9568 mL	1.9136 mL	9.5681 mL
20 mM	0.0957 mL	0.4784 mL	0.9568 mL	4.7840 mL
50 mM	0.0383 mL	0.1914 mL	0.3827 mL	1.9136 mL
100 mM	0.0191 mL	0.0957 mL	0.1914 mL	0.9568 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc