Pricing Availability   Qty
Description: High affinity and reversible P2Y12 antagonist; displays inverse agonism in vitro; also inhibits ENT1
Chemical Name: (1S,2S,3R,5S)-3-[7-[[(1R,2S)-2-(3,4-Difluorophenyl)cyclopropyl]amino]-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)-1,2-cyclopentanediol
Purity: ≥98% (HPLC)
Citations (1)
Literature (5)

Biological Activity for Ticagrelor

Ticagrelor is a high affinity and reversible P2Y12 antagonist (pKi = 8.7) that displays inverse agonism in 1321N1 cells. Also high affinity inhibitor of equilibrative nucleoside transporter 1 (ENT1; Ki = 41 nM). Inhibits ADP-induced platelet aggregation.

Technical Data for Ticagrelor

M. Wt 522.57
Formula C23H28F2N6O4S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 274693-27-5
PubChem ID 9871419
Smiles CCCSC1=NC(N[C@@H]2C[C@H]2C2=CC(F)=C(F)C=C2)=C2N=NN([C@@H]3C[C@H](OCCO)[C@@H](O)[C@H]3O)C2=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Ticagrelor

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 52.26 100
ethanol 26.13 50

Preparing Stock Solutions for Ticagrelor

The following data is based on the product molecular weight 522.57. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.91 mL 9.57 mL 19.14 mL
5 mM 0.38 mL 1.91 mL 3.83 mL
10 mM 0.19 mL 0.96 mL 1.91 mL
50 mM 0.04 mL 0.19 mL 0.38 mL

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References for Ticagrelor

References are publications that support the biological activity of the product.

Springthorpe et al (2007) From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis. Bioorg.Med.Chem.Letts. 17 6013 PMID: 17827008

Aungraheeta et al (2016) Inverse agonism at the P2Y12 receptor and ENT1 transporter blockade contribute to platelet inhibition by ticagrelor. Blood. 128 2717 PMID: 27694321

Armstrong et al (2014) Characterization of the adenosine pharmacology of ticagrelor reveals therapeutically relevant inhibition of equilibrative nucleoside transporter 1. J.Cardiovasc.Pharmacol.Ther. 19 209 PMID: 24414167

If you know of a relevant reference for Ticagrelor, please let us know.

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Keywords: Ticagrelor, Ticagrelor supplier, high, affinity, purinergic, P2Y12, receptor, antagonists, inverse, agonists, antagonism, agonism, ENT1, inhibitors, inhibits, equilibrative, nucleoside, transporter, antagonises, Purinergic, P2Y, Receptors, Nucleoside, Transporters, 6864, Tocris Bioscience

1 Citation for Ticagrelor

Citations are publications that use Tocris products. Selected citations for Ticagrelor include:

Li et al (2020) P2Y12 shRNA normalizes inflammatory dysfunctional hepatic glucokinase activity in type 2 diabetic rats. Biomed.Pharmacother. 132 110803 PMID: 33017768

Do you know of a great paper that uses Ticagrelor from Tocris? Please let us know.

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Literature in this Area

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