Ticagrelor is the first reversibly binding oral P2Y₁₂ platelet receptor antagonist, featuring a complex cyclopentane-triazolopyrimidine structure with multiple stereocentres. Structurally, Ticagrelor consists of a triazolo[4,5-d]pyrimidine core with a propylthio substituent at the 5-position, a cyclopropylamino group at the 7-position, and a cyclopentane ring bearing three hydroxyl groups and a hydroxyethoxy substituent.
Ticagrelor is a reversible, direct-acting P2Y₁₂ receptor antagonist indicated for the prevention of atherothrombotic events in patients with acute coronary syndrome (ACS) and coronary artery disease. As the first agent in its class that does not require metabolic activation, Ticagrelor provides rapid onset and offset of platelet inhibition, with 100% inhibition of platelet aggregation achieved at therapeutic doses. Ticagrelor and its major active metabolite, AR-C124910XX, are approximately equipotent and together contribute to the drug's antiplatelet effect. Ticagrelor and its related impurities—including AR-C124910XX, AR-C133913XX, and various metabolites—serve as critical reference standards for analytical method development, method validation (AMV), and quality control (QC) in ANDA filings.
Product Parameters
Parameter
Specification
Product Name
Ticagrelor
CAS Number
274693-27-5
Molecular Formula
C₂₃H₂₈F₂N₆O₄S
Molecular Weight
522.57 g/mol
Appearance
White to off-white solid
Solubility
Soluble in DMSO
Storage Condition
Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
Mechanism of action
Ticagrelor is an oral, reversible, fast-acting P2Y12 receptor antagonist that exerts therapeutic effects by inhibiting platelet activation.
Efficacy and Uses
Ticagrelor is a platelet aggregation inhibitor that can be used to prevent stroke and myocardial infarction in patients with acute coronary syndrome. As a non-prodrug, it takes effect directly without metabolic activation by the liver, and binds reversibly to the P2Y12 ADP receptor. Research results show that 12-month treatment with ticagrelor, without increasing major bleeding, further significantly reduces the risk of the composite endpoint of cardiovascular death/myocardial infarction/stroke in patients with acute coronary syndrome (ACS) by 16% compared with clopidogrel, and significantly reduces cardiovascular death by 21% at the same time.
Side Effect
The most commonly reported adverse reactions are dyspnea, contusion and epistaxis; other common adverse reactions are: gastrointestinal bleeding, subcutaneous or dermal bleeding, ecchymosis, and bleeding at the operation site.
Contact Us
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