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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)
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 |
| InChI Key | OEKWJQXRCDYSHL-FNOIDJSQSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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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Product Datasheets for Ticagrelor
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
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