Cat. No.: HY-10064

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Ticagrelor

(Synonyms: AZD6140; AR-C 126532XX)

11 Cited Publications

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Based on 11 publication(s) in Google Scholar

Ticagrelor (AZD6140) is a reversible oral P2Y12 receptor antagonist for the treatment of platelet aggregation.

For research use only. We do not sell to patients.

Purity: 99.95%
CAS No.: 274693-27-5
Formula: C₂₃H₂₈F₂N₆O₄S
Molecular Weight:522.57

Storage:

-20°C, protect from light, stored under nitrogen

* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light, stored under nitrogen)

Ticagrelor Chemical Structure

CAS No.: 274693-27-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (11)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

Ticagrelor (AZD6140) is a reversible oral P2Y12 receptor antagonist for the treatment of platelet aggregation.

IC₅₀ & Target

P2Y12 Receptor

All P2Y Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Platelet	IC₅₀	0.74 μM Compound: Ticagrelor	Antiplatelet activity against ADP-induced human platelet in platelet rich plasma assessed as inhibition of platelet aggregation preincubated for 2 mins followed by ADP stimulation and measured for 5 mins by aggregometry Antiplatelet activity against ADP-induced human platelet in platelet rich plasma assessed as inhibition of platelet aggregation preincubated for 2 mins followed by ADP stimulation and measured for 5 mins by aggregometry	[PMID: 34458743]
Platelet	IC₅₀	1.83 μM Compound: 1, AZD-6140	Inhibition of ADP-stimulated platelet aggregation in human platelet rich plasma by 96-well format based turbidimetric method Inhibition of ADP-stimulated platelet aggregation in human platelet rich plasma by 96-well format based turbidimetric method	[PMID: 22984835]
Platelet	IC₅₀	2 μM Compound: Ticagrelor	Inhibition of collagen-induced platelet aggregation in human platelet preincubated for 5 mins followed by collagen-stimulation and measured after 6 mins by lumi-aggregometric method Inhibition of collagen-induced platelet aggregation in human platelet preincubated for 5 mins followed by collagen-stimulation and measured after 6 mins by lumi-aggregometric method	[PMID: 32155530]
Platelet	IC₅₀	4 μM Compound: Ticagrelor	Inhibition of TRAP6-induced platelet aggregation in human platelet preincubated for 5 mins followed by TRAP6-stimulation and measured after 6 mins by lumi-aggregometric method Inhibition of TRAP6-induced platelet aggregation in human platelet preincubated for 5 mins followed by TRAP6-stimulation and measured after 6 mins by lumi-aggregometric method	[PMID: 32155530]

In Vitro

Ticagrelor promotes a greater inhibition of adenosine 5′-diphosphate (ADP)-induced Ca²⁺ release in ished platelets vs other P2Y12R antagonists. This additional effect of ticagrelor beyond P2Y12R antagonism is in part as a consequence of ticagrelor inhibiting the equilibrative nucleoside transporter 1 (ENT1) on platelets, leading to accumulation of extracellular adenosine and activation of Gs-coupled adenosine A2A receptors^[1]. B16-F10 cells exhibit decreased interaction with platelets from ticagrelor-treated mice compared to saline-treated mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In B16-F10 melanoma intravenous and intrasplenic metastasis models, mice treated with a clinical dose of ticagrelor (10 mg/kg) exhibits marked reductions in lung (84%) and liver (86%) metastases. Furthermore, ticagrelor treatment improves survival compared to saline-treated animals. A similar effect is observed in a 4T1 breast cancer model, with reductions in lung (55%) and bone marrow (87%) metastases following ticagrelor treatment^[2]. Single oral administration of ticagrelor (1-10 mg/kg) causes dose-related inhibitory effect on platelet aggregation. Ticagrelor, at the highest dose (10 mg/kg) significantly inhibits platelet aggregation at 1 h after dosing and the peak inhibition is observed at 4 h after dosing^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 274693-27-5
Appearance Solid
Molecular Weight 522.57
Formula C₂₃H₂₈F₂N₆O₄S
Color White to yellow
SMILES

O[C@H]1[C@@H](O)[C@H](N2N=NC3=C(N[C@H]4[C@H](C5=CC=C(F)C(F)=C5)C4)N=C(SCCC)N=C32)C[C@@H]1OCCO
Synonyms

AZD6140; AR-C 126532XX
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light, stored under nitrogen)

Publications (11)

All Bio/Physico-chemical AssayIn Vivo Efficacy StudyRT-PCRWBCell Imaging/Staining

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Journal Impact Factor

Cell Res

The axon initial segment-associated microglia regulate neuronal activity and visual perception. [Abstract]

2026 Jan 28. PMID: 41593328
Microsyst Nanoeng

High-throughput combinatorial screening of antiplatelet drugs for personalized medicine. [Abstract]

2026 Jan 1;12(1):7. PMID: 41476049

Ticagrelor purchased from MedChemExpress. Usage Cited in: Microsyst Nanoeng. 2026 Jan 1;12(1):7. [Abstract]

Ticagrelor (0–20 µM) showed anti-aggregation effects, with an IC₅₀ value of 0.9242 µM in healthy human platelets.
Curr Biol

Microglia modulate general anesthesia through P2Y12 receptor. [Abstract]

2023 Jun 5;33(11):2187-2200.e6. PMID: 37167975
Biochem Pharmacol

Ticagrelor reverses multidrug resistance in breast cancer by inhibiting PI3K/AKT/mTOR pathway and suppressing ABCB1 expression and function. [Abstract]

2026 Mar 15:249:117903. PMID: 41846011
Mol Neurobiol

Study of the Involvement of the P2Y12 Receptor in Chronic Itching in Type 2 Diabetes Mellitus. [Abstract]

2022 Mar;59(3):1604-1618. PMID: 35000152

Ticagrelor purchased from MedChemExpress. Usage Cited in: Mol Neurobiol. 2022 Mar;59(3):1604-1618. [Abstract]

After intraperitoneal injection of STZ, body weight was significantly decreased, whereas it was increased following intraperitoneal injection of P2Y12 shRNA or intragastric administration of ticagrelor (intragastric administration，100 mg/kg, 1 week).

Ticagrelor purchased from MedChemExpress. Usage Cited in: Mol Neurobiol. 2022 Mar;59(3):1604-1618. [Abstract]

Fasting blood glucose (FBG) was decreased after intrathecal injection of P2Y12 shRNA or intragastric administration of ticagrelor (100 mg/kg, 1 week) in type 2 diabetic mice.

Ticagrelor purchased from MedChemExpress. Usage Cited in: Mol Neurobiol. 2022 Mar;59(3):1604-1618. [Abstract]

P2Y12 shRNA or ticagrelor (intragastric administration, 100 mg/kg, 1 week) alleviated cold hyperalgesia, thermal hyperalgesia, spontaneous itching behaviour, and sciatic nerve conduction velocity (SNCV) deficits in mice. (a) The number of paw lifts on a cold plate within 5 min. (b) Paw withdrawal latency in the hot plate test. (c) Number of spontaneous scratches within 30 min. (d) Sciatic nerve conduction velocity. Data are presented as mean ± SD (n = 8 per group). *p < 0.05, **p < 0.01 vs. control; ##p < 0.01 vs. DMI (type 2 diabetes mellitus + itch model).

Ticagrelor purchased from MedChemExpress. Usage Cited in: Mol Neurobiol. 2022 Mar;59(3):1604-1618. [Abstract]

Ticagrelor (intragastric administration, 100 mg/kg, 1 week) inhibited the expression of P2Y12 mRNA in the dorsal root ganglia (DRG) of mice in the type 2 diabetes mellitus + itch model group.

Ticagrelor purchased from MedChemExpress. Usage Cited in: Mol Neurobiol. 2022 Mar;59(3):1604-1618. [Abstract]

Ticagrelor (intragastric administration, 100 mg/kg, 1 week) inhibited the expression of P2Y12 protein in the DRG of mice in the type 2 diabetes mellitus + itch model group.

Ticagrelor purchased from MedChemExpress. Usage Cited in: Mol Neurobiol. 2022 Mar;59(3):1604-1618. [Abstract]

Ticagrelor (intragastric administration, 100 mg/kg, 1 week) reduced reactive oxygen species (ROS) levels in the DRG of mice in the type 2 diabetes mellitus + itch model group.
Heliyon

Novel cancer-fighting role of ticagrelor inhibits GTSE1-induced EMT by regulating PI3K/Akt/NF-κB signaling pathway in malignant glioma. [Abstract]

2024 May 7;10(9):e30833. PMID: 38774096
Clin Chim Acta

Simultaneous quantification of acetylsalicylic acid, clopidogrel, ticagrelor and their major metabolites in human plasma by liquid chromatography-tandem mass spectrometry. [Abstract]

2025 Dec 31:120816. PMID: 41482259
Chem Biodivers

UPLC-QTOF-MS-Based Quantification and Antiplatelet Activity Evaluation of Herb Pair Interactions Between Red Ginseng and Trogopterus Feces. [Abstract]

2025 Apr 23:e202500770. PMID: 40265573
Biomed Res Int

Hemostatic Effect of 20(S)-Panaxadiol by Induced Platelet Aggregation Depending on Calcium Signaling Pathway. [Abstract]

2022 Sep 20;2022:8265898. PMID: 36177062
Orebro University

2024.
Research Square Preprint

2021 Mar.

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (95.68 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9136 mL

9.5681 mL

19.1362 mL

5 mM

0.3827 mL

1.9136 mL

3.8272 mL

10 mM

0.1914 mL

0.9568 mL

1.9136 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light, stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2 mg/mL (3.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2 mg/mL (3.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2 mg/mL (3.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Animal Administration^[3]

Rats: Prasugrel (10 mg/kg, p.o.) and ticagrelor (30 mg/kg, p.o.), doses that produced similar levels of inhibition of platelet aggregation, are administered to rats 4 h before the bleeding time measurements. Fresh, washed platelets (1 × 1010 platelets/mL) are prepared from other rats and suspended in Hank's balanced salt solution. Platelets are transfused via the jugular vein to rats 1 h before the bleeding time measurements and the bleeding time is determined^[3].

^[2]Mice: Female BALB/c mice are inoculated subcutaneously in the fourth mammary pad with 4T1 breast cancer cells. Once a tumor is palpable, mice receive daily injections of PBS or ticagrelor (10 mg/kg). One week later, mice undergo primary tumor resection. At 28 days mice are sacrificed and lungs, femurs and tibiae harvested. Dissociated cells from lung and bone marrow are plated in medium containing 60 μM 6-thioguanine. After 14 days, culture plates are fixed with methanol and stained with 0.03% methylene blue to enumerate metastatic 4T1 colonies^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Aungraheeta R, et al. Inverse agonism at the P2Y12 receptor and ENT1 transporter blockade contribute to platelet inhibition by ticagrelor. Blood. 2016 Dec 8;128(23):2717-2728. [Content Brief]

[2]. Gebremeskel S, et al. The reversible P2Y12 inhibitor ticagrelor inhibits metastasis and improves survival in mouse models of cancer. Int J Cancer. 2015 Jan 1;136(1):234-40. [Content Brief]

[3]. Sugidachi A, et al. A comparison of the pharmacological profiles of prasugrel and ticagrelor assessed by platelet aggregation, thrombus formation and haemostasis in rats. Br J Pharmacol. 2013 May;169(1):82-9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9136 mL	9.5681 mL	19.1362 mL	47.8405 mL
	5 mM	0.3827 mL	1.9136 mL	3.8272 mL	9.5681 mL
	10 mM	0.1914 mL	0.9568 mL	1.9136 mL	4.7840 mL
	15 mM	0.1276 mL	0.6379 mL	1.2757 mL	3.1894 mL
	20 mM	0.0957 mL	0.4784 mL	0.9568 mL	2.3920 mL
	25 mM	0.0765 mL	0.3827 mL	0.7654 mL	1.9136 mL
	30 mM	0.0638 mL	0.3189 mL	0.6379 mL	1.5947 mL
	40 mM	0.0478 mL	0.2392 mL	0.4784 mL	1.1960 mL
	50 mM	0.0383 mL	0.1914 mL	0.3827 mL	0.9568 mL
	60 mM	0.0319 mL	0.1595 mL	0.3189 mL	0.7973 mL
	80 mM	0.0239 mL	0.1196 mL	0.2392 mL	0.5980 mL

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Ticagrelor

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Publications Citing Use of MedChemExpress (MCE) Ticagrelor

All P2Y Receptor Isoforms

Biological Activity

Chemical Information

Publications (11)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Ticagrelor Related Classifications

Cat. No.: HY-10064