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Submit ReviewAR-C 69931 tetrasodium salt is a highly potent P2Y12 antagonist (IC50 = 0.4 nM). Inhibits ADP-induced human platelet aggregation ex vivo. Reduces thrombus weight and delays thrombus formation in a model of carotid artery thrombosis in vivo.
分子量 | 864.29 |
公式 | C17H21Cl2F3N5Na4O12P3S2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 163706-36-3 |
PubChem ID | 10260031 |
InChI Key | COWWROCHWNGJHQ-OPKBHZIBSA-J |
Smiles | O[C@@H]1[C@H](O)[C@@H](N2C3=NC(SCCC(F)(F)F)=NC(NCCSC)=C3N=C2)O[C@H]1COP(OP(C(Cl)(Cl)P(O[Na])(O[Na])=O)(O[Na])=O)(O[Na])=O |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 86.43 | 100 |
以下数据基于产品分子量 864.29。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.16 mL | 5.79 mL | 11.57 mL |
5 mM | 0.23 mL | 1.16 mL | 2.31 mL |
10 mM | 0.12 mL | 0.58 mL | 1.16 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
参考文献是支持产品生物活性的出版物。
Huang et al (2000) Prevention of arterial thrombosis by intravenously administered platelet P2T receptor antagonist AR-C69931MX in a canine model. J.Pharmacol.Exp.Ther. 295 492 PMID: 11046080
Ingall et al (1999) Antagonists of the platelet P2T receptor: a novel approach to antithrombotic therapy. J.Med.Chem. 42 213 PMID: 9925726
Srinivasan et al (2009) The P2Y12 antagonists, 2-methylthioadenosine 5'-monophosphate triethylammonium salt and cangrelor (ARC69931MX), can inhibit human platelet aggregation through a Gi-independent increase in cAMP levels. J.Biol.Chem. 284 16108 PMID: 19346255
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关键词: AR-C 69931 tetrasodium salt, AR-C 69931 tetrasodium salt supplier, ARC69931, tetrasodium, salt, P2Y12, P2T, potent, purinergic, antagonists, antagonism, antithrombotic, antagonises, inhibitors, inhibits, Cangrelor, Purinergic, P2Y, Receptors, 5720, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 AR-C 69931 tetrasodium salt 的部分引用包括:
Chris et al (2020) Neuronal hyperexcitability is a DLK-dependent trigger of herpes simplex virus reactivation that can be induced by IL-1. Elife 9 PMID: 33350386
Vivek et al (2020) Three-dimensional growth of breast cancer cells potentiates the anti-tumor effects of unacylated ghrelin and AZP-531. Elife 9 PMID: 32667883
Yu et al (2020) Cancer associated fibroblast FAK regulates malignant cell metabolism. Nat Commun 11 1290 PMID: 32157087
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
Sally et al (2019) Promiscuous G-Protein-Coupled Receptor Inhibition of Transient Receptor Potential Melastatin 3 Ion Channels by Gβγ Subunits. J Neurosci 39 7840-7852 PMID: 31451581
H C et al (2000) Activation of group II metabotropic glutamate receptors induces long-term depression of synaptic transmission in the rat amygdala. J Neurosci 20 9017-24 PMID: 11124977
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