Ticagrelor

Discontinued Product

Ticagrelor (Cat. No. 6864) has been withdrawn from sale for commercial reasons.
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)
Datasheet
Citations (1)
Reviews
Literature (1)

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.

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

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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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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


P2X and P2Y Receptors Scientific Review

P2X and P2Y Receptors Scientific Review

Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.