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Submit ReviewAR-C 66096 tetrasodium salt is a potent and selective P2Y12 receptor antagonist. Blocks ADP-induced inhibition of adenylyl cyclase in vitro (pKB =7.6) and inhibits ADP-induced aggregation of washed human platelets (pIC50 = 8.16).
Sold for research purposes under agreement from AstraZeneca
分子量 | 703.26 |
公式 | C14H18F2N5Na4O12P3S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 145782-74-7 |
PubChem ID | 90488830 |
InChI Key | IETVOLFQZIGNAQ-HVYRMSERSA-J |
Smiles | [Na+].[Na+].[Na+].[Na+].CCCSC1=NC(N)=C2N=CN([C@@H]3O[C@H](COP([O-])(=O)OP([O-])(=O)C(F)(F)P([O-])([O-])=O)[C@@H](O)[C@H]3O)C2=N1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Humphries et al (1994) FPL 66096: a novel, highly potent and selective antagonist at human platelet P2T-purinoceptors. Br.J.Pharmacol. 113 1057 PMID: 7858849
Ingall et al (1999) Antagonists of the platelet P receptor: a novel approach to antithrombotic therapy. J.Med.Chem. 42 213 PMID: 9925726
Simon et al (2001) Activity of adenosine diphosphates and triphosphates on a P2YT-type receptor in brain capillary endothelial cells. Br.J.Pharmacol. 132 173 PMID: 11156575
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引用文献是使用了 Tocris 产品的出版物。 AR-C 66096 tetrasodium salt 的部分引用包括:
Zhang et al (2014) Agonist-bound structure of the human P2Y12 receptor. Purinergic Signal 509 119 PMID: 24784220
Gao et al (2013) The role of P2Y(14) and other P2Y receptors in degranulation of human LAD2 mast cells. Cell Commun Signal 9 31 PMID: 22825617
Helms et al (2013) Mechanisms of hemolysis-associated platelet activation. J Thromb Haemost 11 2148 PMID: 24119131
Pinheiro et al (2013) Bradykinin-induced Ca2+ signaling in human subcutaneous fibroblasts involves ATP release via hemichannels leading to P2Y12 receptors activation. Cell Commun Signal 11 70 PMID: 24047499
Aungraheeta et al (2016) Inverse agonism at the P2Y12 receptor and ENT1 transporter blockade contribute to platelet inhibition by ticagrelor. Blood 128 2717 PMID: 27694321
Lu et al (2018) The P2Y12 Receptor Antagonist Ticagrelor Reduces Lysosomal pH and Autofluorescence in Retinal Pigmented Epithelial Cells From the ABCA4-/- Mouse Model of Retinal Degeneration. Front Pharmacol 9 242 PMID: 29725296
Chan et al (2018) Not all light transmission aggregation assays are created equal: qualitative differences between light transmission and 96-well plate aggregometry. Platelets 29 686 PMID: 29715047
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