Ticagrelor

SKU: orb1310865

Description

Ticagrelor is a direct-acting, reversible P2Y12 receptor antagonist that inhibits platelet aggregation. It is widely used in cardiovascular disease research, with applications in both in vitro platelet function studies and in vivo models of thrombosis and acute coronary syndromes.

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 274693-27-5
• MW: 522.57
• Purity: >99.99% (May vary between batches)
• Formula: C₂₃H₂₈F₂N₆O₄S
• SMILES: CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(F)c(F)c2)c2nnn([C@@H]3C[C@H](OCCO)[C@@H](O)[C@H]3O)c2n1
• Target: Cytochromes P450,P2Y Receptor
• Solubility: DMSO:250 mg/mL (478.4 mM);5% DMSO+40 % PEG300+5 % Tween 80+50 % Saline:5 mg/mL (9.57 mM)

Bioactivity

• Target IC50:
  P2Y12:2 nM(Ki)
• In Vivo:
  In binding studies on CHO-K1 cells transfected with rh-P2Y12 receptors, Ticagrelor exhibited efficient and reversible binding, with a kon (association rate constant) of 0.00011/(nM·s), a Kd (equilibrium dissociation constant) of 10.5 nM, and a koff (dissociation rate constant) of 0.00087/s. The half-lives for association and dissociation were 4 and 14 minutes, respectively, suggesting that the concentration of the drug that binds to platelets determines the extent of platelet inhibition. Ticagrelor is an active drug that does not require metabolic activation. It does not directly compete with ADP at the ADP binding site but rather occupies a nearby site, causing a change in the conformation of the binding site that leads to a reversible conformational change in the receptor. The binding of Ticagrelor to the receptor is reversible with quick onset/off rates.
• In Vitro:
  Ticagrelor has a half-life (t1/2) of approximately 7-8.5 hours and exhibits a dose-related inhibition of platelet aggregation; a 100-400 mg dose achieves complete inhibition within 2 hours. It is well-tolerated, with no serious adverse events or significant changes in laboratory values observed. Ticagrelor is rapidly absorbed, reaching peak levels in 1.3-2 hours. Within the studied dosage range, both the peak concentration of Ticagrelor and the area under the curve (from time zero to infinity) increase in a dose-proportional manner, indicating linear pharmacokinetics.

Storage & Handling

• Storage: keep away from moisture | Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ticagrelor, CYP2C9, AZD6140, AZD-6140, AZD 6140, AR-C 126532XX, inhibit, P2YReceptor, P2Y12, P2Y Receptor, P2Y, Inhibitor

Compound Identifiers

PubChem CID

9871419