Ticagrelor 99% Purity P2Y12 Receptor Antagonist CAS 274693-27-5 Antiplatelet API Pharmaceutical Grade

Product Overview

Ticagrelor is an orally active, reversible P2Y12 receptor antagonist used for the prevention of thrombotic events in patients with acute coronary syndrome (ACS) and a history of myocardial infarction. Marketed under the brand name Brilinta (Brilique in Europe), ticagrelor was the first reversible oral P2Y12 inhibitor approved by the FDA in July 2011. Unlike thienopyridines such as clopidogrel, ticagrelor binds reversibly to the P2Y12 receptor, providing rapid onset and offset of antiplatelet effect, and does not require metabolic activation. It has demonstrated superior efficacy compared to clopidogrel in reducing cardiovascular events in ACS patients.

Chemically, ticagrelor is (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)cyclopentane-1,2-diol with the molecular formula C₂₃H₂₈F₂N₆O₄S and a molecular weight of 522.57 g/mol. It is a white to off-white crystalline powder with solubility in DMSO and methanol. The compound exhibits high selectivity for the P2Y12 receptor and favorable pharmacokinetic properties.

Mechanism of Action

Ticagrelor exerts its antiplatelet effect through reversible P2Y12 receptor antagonism:

• Reversible P2Y12 Inhibition: Binds reversibly to the platelet P2Y12 receptor, preventing ADP-mediated platelet activation and aggregation

• Rapid Onset and Offset: Fast onset of action (peak effect within 2 hours) and rapid offset (platelet function recovery within 3-5 days), advantages for patients requiring surgery

• No Metabolic Activation: Directly active, unlike clopidogrel which requires CYP450 metabolism, avoiding variability due to genetic polymorphisms

• Additional Effects: May have additional pleiotropic effects including improvements in endothelial function and reduced inflammation

• Dose-dependent Effect: Produces predictable, dose-dependent inhibition of platelet aggregation

Research Applications & Market Significance

Ticagrelor has become a standard of care in acute coronary syndrome and is expanding into new indications:

• Acute Coronary Syndrome: First-line antiplatelet therapy for ST-elevation and non-ST elevation myocardial infarction

• Secondary Prevention: Long-term secondary prevention in patients with a history of myocardial infarction

• Stroke Prevention: Approved for secondary prevention of ischemic stroke and transient ischemic attack

• Peripheral Artery Disease: Emerging indication in patients with peripheral artery disease

• Combination Therapy: Used in combination with aspirin for dual antiplatelet therapy (DAPT)

• Shorter DAPT Duration: Research supporting shorter DAPT duration with ticagrelor monotherapy after ACS

The global antiplatelet market is expected to exceed $15 billion by 2028, driven by increasing prevalence of cardiovascular diseases and growing adoption of newer antiplatelet agents. Ticagrelor continues to gain market share from clopidogrel due to its superior efficacy and reversible mechanism of action.

Quality Specifications

Our ticagrelor is manufactured under strict GMP conditions and meets international pharmacopeia standards:

• Purity: ≥99.0% determined by HPLC

• Identity confirmed by NMR, mass spectrometry, and infrared spectroscopy

• Water content: ≤0.5%

• Residual solvents: Meet ICH Q3C guidelines

• Heavy metals: ≤10 ppm

• Related substances: Each impurity ≤0.1%, total impurities ≤0.5%

• Enantiomeric purity: ≥99.8% ee

• Residue on ignition: ≤0.1%

• Each batch accompanied by comprehensive Certificate of Analysis (COA)

• Stable for 36 months when stored at room temperature in sealed containers

Packaging & Shipping

We offer flexible packaging options to meet diverse customer needs:

• Small quantities: 1kg, 5kg aluminum foil bags

• Bulk quantities: 25kg fiber drums with PE liners

• Custom packaging available upon request

• GMP-grade packaging available for pharmaceutical customers

• Shipped at ambient temperature

• International shipping with proper documentation

• MSDS and COA provided with each shipment