Ticagrelor (Synonyms: AZD6140; AR-C 126532XX)

Name: Ticagrelor
Brand: MedChemExpress
SKU: HY-10064
Rating: 5.0 (11 reviews)

Cat. No.: HY-10064 Purity: 99.95%: Data Sheet
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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.

CAS No. : 274693-27-5

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Ticagrelor:

11 Publications Citing Use of MCE Ticagrelor

Bio/Physico-chemical Assay

In Vivo Efficacy Study

RT-PCR

Cell Imaging/Staining

: 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.

: 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.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target

P2Y12 Receptor

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

Molecular Weight

522.57

Formula

C₂₃H₂₈F₂N₆O₄S

CAS No.

274693-27-5

Appearance

Solid

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

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)

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (281 KB) SDS (396 KB)

COA (253 KB) LCMS (93 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]

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].

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

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]

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

Ticagrelor Related Classifications

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ticagrelor274693-27-5AZD6140AR-C 126532XXAZD 6140AZD-6140P2Y ReceptorInhibitorinhibitorinhibit

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Ticagrelor (Synonyms: AZD6140; AR-C 126532XX)

Customer Review

Other Forms of Ticagrelor:

Ticagrelor Related Antibodies

11 Publications Citing Use of MCE Ticagrelor

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•Related Screening Libraries:

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View All P2Y Receptor Isoform Specific Products:

Biological Activity

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Purity & Documentation

References

Customer Review

Ticagrelor Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Ticagrelor Related Classifications

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