Ticagrelor

Name: Ticagrelor
Brand: Tocris Bioscience
SKU: 6864
Price: 49 USD

Catalog #: 6864
1 Citation Datasheet / COA / SDS

Discontinued Product

6864 has been discontinued.

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Ticagrelor | CAS No. 274693-27-5 | P2Y Receptor Antagonists

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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%

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Product Details

Citations (1)

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Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

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

Technical Data

M.Wt:

522.57

Formula:

C₂₃H₂₈F₂N₆O₄S

Solubility:

Soluble to 100 mM in DMSO and to 50 mM in ethanol

Purity:

≥98%

Storage:

Store at -20°C

CAS No:

274693-27-5

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.

Background References

From ATP to AZD6140: the discovery of an orally active reversible P2Y₁₂ receptor antagonist for the prevention of thrombosis.
Springthorpe et al.
Bioorg.Med.Chem.Letts., 2007;17:6013
Inverse agonism at the P2Y₁₂ receptor and ENT1 transporter blockade contribute to platelet inhibition by ticagrelor.
Aungraheeta et al.
Blood., 2016;128:2717
Characterization of the adenosine pharmacology of ticagrelor reveals therapeutically relevant inhibition of equilibrative nucleoside transporter 1.
Armstrong et al.
J.Cardiovasc.Pharmacol.Ther., 2014;19:209

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Citation for Ticagrelor

The citations listed below are publications that use Tocris products. Selected citations for Ticagrelor include:

1 Citation: Showing 1 - 1

P2Y12 shRNA normalizes inflammatory dysfunctional hepatic glucokinase activity in type 2 diabetic rats.
Authors: Li Et al.
Biomed.Pharmacother. 2020;132:110803

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