Cangrelor tetrasodium - CAS 163706-36-3
Catalog number: B0084-468043
Category: Inhibitor
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P2Y Receptor
Cangrelor tetrasodium is an ATP analogue and acts as a reversible antagonist of P2Y12 receptor. Pretreatment with cangrelor significantly reduces blood clotting induced by ADP in a mouse model of pulmonary thromboembolism.
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B0084-468043 10 mg $199 In stock
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Brife Description:
P2Y12 receptor antagonist
Cangrelor Tetrasodium; AR-C69931MX; AR C69931MX; ARC69931MX; N6-(2-Methylthioethyl)-2-(3,3,3-trifluoropropylthio)-betagamma-dichloromethylene-ATP tetrasodium salt
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1.Dependence of platelet thrombus stability on sustained glycoprotein IIb/IIIa activation through adenosine 5'-diphosphate receptor stimulation and cyclic calcium signaling.
Goto S;Tamura N;Ishida H;Ruggeri ZM J Am Coll Cardiol. 2006 Jan 3;47(1):155-62. Epub 2005 Dec 15.
OBJECTIVES: ;We sought to evaluate the mechanisms that support the stability of platelet aggregates on a thrombogenic surface exposed to flowing blood.;BACKGROUND: ;Activation of the membrane glycoprotein (GP) IIb/IIIa--mediated in part through the P2Y1 and P2Y12 adenosine 5'-diphosphate (ADP) receptors--is necessary for platelet aggregation. Platelets in growing thrombi exhibit cyclic calcium signal, suggesting that sustained activation may be required for thrombus stability.;METHODS: ;Blood was perfused over type I collagen fibrils at the wall shear rate of 1,500 s(-1). Three-dimensional visualization of platelet thrombi was obtained in real time with confocal microscopy. The intracytoplasmic Ca2+ concentration ([Ca2+]i) was measured in fluo-3AM-loaded platelets.;RESULTS: ;The height of platelet thrombi in control blood was 13.5 +/- 3.3 microm after 6 min, and increased to 16.3 +/- 4.5 microm (n = 8) after an additional 6 min. In contrast, the height was reduced to 5.4 +/- 2.2 and 3.3 +/- 1.3 microm, respectively (p < 0.01, n = 8), when the blood used in the second 6-min perfusion contained a P2Y1 (MRS2179) or P2Y12 (AR-C69931MX) inhibitor. The [Ca2+]i of platelets within forming thrombi oscillated between 212 +/- 38 nmol/l and 924 +/- 458 nmol/l, with cycles lasting 4.
2.Lipid rafts are essential for release of phosphatidylserine-exposing extracellular vesicles from platelets.
Wei H;Malcor JM;Harper MT Sci Rep. 2018 Jul 3;8(1):9987. doi: 10.1038/s41598-018-28363-4.
Platelets protect the vascular system during damage or inflammation, but platelet activation can result in pathological thrombosis. Activated platelets release a variety of extracellular vesicles (EVs). EVs shed from the plasma membrane often expose phosphatidylserine (PS). These EVs are pro-thrombotic and increased in number in many cardiovascular and metabolic diseases. The mechanisms by which PS-exposing EVs are shed from activated platelets are not well characterised. Cholesterol-rich lipid rafts provide a platform for coordinating signalling through receptors and Ca;2+; channels in platelets. We show that cholesterol depletion with methyl-β-cyclodextrin or sequestration with filipin prevented the Ca;2+;-triggered release of PS-exposing EVs. Although calpain activity was required for release of PS-exposing, calpain-dependent cleavage of talin was not affected by cholesterol depletion. P2Y;12; and TPα, receptors for ADP and thromboxane A;2;, respectively, have been reported to be in platelet lipid rafts. However, the P2Y;12; antagonist, AR-C69931MX, or the cyclooxygenase inhibitor, aspirin, had no effect on A23187-induced release of PS-exposing EVs. Together, these data show that lipid rafts are required for release of PS-exposing EVs from platelets.
3.Pharmacodynamic profile of antiplatelet agents: marked differences between single versus costimulation with platelet activators.
Graff J;Klinkhardt U;Harder S Thromb Res. 2004;113(5):295-302.
BACKGROUND: ;In pharmacodynamic studies with antiplatelet agents, platelets are usually activated in vitro with single agonists (e.g., ADP) solely. We questioned whether differences occur between single and combined stimulation of platelets [involving the major thrombin-receptors, protease-activated receptors (PAR)1 and PAR4], and whether the pharmacodynamic response to common antiplatelet drugs vary when a combined stimulus is applied instead of a single agonist.;METHODS: ;We investigated the influence of different antiplatelet agents (aspirin [500 mg]) in vivo, the P2Y12-antagonist AR-C 69931MX (4 nM) and the GPII/IIIa-antagonist (abciximab ([5 microg/ml] in vitro) on the degranulation response (CD62) and expression of the activated GPIIb/IIIa-receptor (PAC-1) after stimulation with ADP (2 microM), collagen (4 microg/ml), a PAR1-activating peptide (3 microM TRAP) and a PAR4-activating peptide (200 microM AYPGKF) alone or in a combination of each two agonists by flow cytometry in healthy subjects.;RESULTS: ;(1) Combined activation of TRAP with AYPGKF resulted in synergistic CD62 and PAC-1 expression. Only AYPGKF but neither TRAP nor ADP acted synergistically with collagen. (2) AR-C 69931MX inhibited platelet degranulation (CD62) in all inducer combinations with ADP or the combination TRAP with AYPGKF.
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