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说明： High affinity and reversible P2Y12 antagonist; displays inverse agonism in vitro; also inhibits ENT1
化学名： (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)-1,2-cyclopentanediol
纯度： ≥98% (HPLC)
生物活性 for Ticagrelor
Ticagrelor is a high affinity and reversible P2Y12 antagonist (pKi = 8.7) that displays inverse agonism in 1321N1 cells. Also high affinity inhibitor of equilibrative nucleoside transporter 1 (ENT1; Ki = 41 nM). Inhibits ADP-induced platelet aggregation.
技术数据 for Ticagrelor
| 分子量 | 522.57 |
| 公式 | C23H28F2N6O4S |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 274693-27-5 |
| PubChem ID | 9871419 |
| InChI Key | OEKWJQXRCDYSHL-FNOIDJSQSA-N |
| Smiles | CCCSC1=NC(N[C@@H]2C[C@H]2C2=CC(F)=C(F)C=C2)=C2N=NN([C@@H]3C[C@H](OCCO)[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.
产品说明书 for Ticagrelor
参考文献 for Ticagrelor
参考文献是支持产品生物活性的出版物。
Springthorpe et al (2007) From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis. Bioorg.Med.Chem.Letts. 17 6013 PMID: 17827008
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
Armstrong et al (2014) Characterization of the adenosine pharmacology of ticagrelor reveals therapeutically relevant inhibition of equilibrative nucleoside transporter 1. J.Cardiovasc.Pharmacol.Ther. 19 209 PMID: 24414167
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关键词: Ticagrelor, Ticagrelor supplier, high, affinity, purinergic, P2Y12, receptor, antagonists, inverse, agonists, antagonism, agonism, ENT1, inhibitors, inhibits, equilibrative, nucleoside, transporter, antagonises, Purinergic, P2Y, Receptors, Nucleoside, Transporters, 6864, Tocris Bioscience
1 篇 Ticagrelor 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Ticagrelor 的部分引用包括：
Li et al (2020) P2Y12 shRNA normalizes inflammatory dysfunctional hepatic glucokinase activity in type 2 diabetic rats. Biomed.Pharmacother. 132 110803 PMID: 33017768
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
P2X and P2Y Receptors Scientific Review
Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.