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Ticagrelor

CAT: 0013-GTR19162426-01Size: 500 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19162426-01Size:500 mg
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Description
A potent, selective, reversible and oral P2Y12 receptor antagonist with pKi of 8.7; effectively inhibits platelet aggregation without significant increases in bleeding time in vivo; is used for the prevention of thrombotic events (for example stroke or heart attack) in people with acute coronary syndrome or myocardial infarction with ST elevation.Thrombosis Approved (In Vitro) :Ticagrelor promotes a greater inhibition of adenosine 5′-diphosphate (ADP) –induced Ca2+ release in ished platelets vs other P2Y12R antagonists. This additional effect of ticagrelor beyond P2Y12R antagonism is in part as a consequence of ticagrelor inhibiting the equilibrative nucleoside transporter 1 (ENT1) on platelets, leading to accumulation of extracellular adenosine and activation of Gs-coupled adenosine A2A receptors. B16-F10 cells exhibit decreased interaction with platelets from ticagrelor-treated mice compared to saline-treated mice. (In Vivo) :In B16-F10 melanoma intravenous and intrasplenic metastasis models, mice treated with a clinical dose of ticagrelor (10 mg/kg) exhibits marked reductions in lung (84%) and liver (86%) metastases. Furthermore, ticagrelor treatment improves survival compared to saline-treated animals. A similar effect is observed in a 4T1 breast cancer model, with reductions in lung (55%) and bone marrow (87%) metastases following ticagrelor treatment. Single oral administration of ticagrelor (1-10 mg/kg) causes dose-related inhibitory effect on platelet aggregation. Ticagrelor, at the highest dose (10 mg/kg) significantly inhibits platelet aggregation at 1 h after dosing and the peak inhibition is observed at 4 h after dosing.
CAS Number
274693-27-5
Product Name Alternative
AR-C 126532XX | AZD 6140 | AZD6140 | AZD-6140
Field of Research
Pharmacology & Drug Discovery
Purity
>98% (HPLC)
Solubility
10 mM in DMSO
Smiles
O[C@H]1[C@@H] (O) [C@H] (N2N=NC3=C (N[C@H]4[C@H] (C5=CC=C (F) C (F) =C5) C4) N=C (SCCC) N=C32) C[C@@H]1OCCO
Molecular Formula
C23H28F2N6O4S
Molecular Weight
522.5681
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
1,2-Cyclopentanediol, 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) -, (1S,2S,3R,5S) -

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