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Submit ReviewNF 023
说明： Selective and competitive P2X1 antagonist
化学名： 8,8'-[carbonylbis(imino-3,1-phenylenecarbonylimino)]bis-1,3,5-naphthalene-trisulphonic acid, hexasodium salt
生物活性 for NF 023
NF 023 is an a subtype-selective, competitive and reversible P2X1 receptor antagonist. Displays IC50 values of 0.21, 28.9, > 50 and > 100 μM for human P2X1, P2X3, P2X2, and P2X4-mediated responses respectively. Selective over adrenoceptors, histamine and P2Y receptors. Also selectively inhibits the α-subunit of Go/i (EC50 ~300 nM). Also inhibits DNA-binding activity of HMGA2 (IC50 = 10.63 μM).
技术数据 for NF 023
| 分子量 | 1162.86 |
| 公式 | C35H20N4Na6O21S6 |
| 储存 | Desiccate at RT |
| CAS Number | 104869-31-0 |
| PubChem ID | 4465 |
| InChI Key | FMQURVHYTBGYSQ-UHFFFAOYSA-H |
| Smiles | [Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[O-]S(=O)(=O)C1=CC2=C(C=CC(NC(=O)C3=CC=CC(NC(=O)NC4=CC(=CC=C4)C(=O)NC4=C5C(C=C(C=C5S([O-])(=O)=O)S([O-])(=O)=O)=C(C=C4)S([O-])(=O)=O)=C3)=C2C(=C1)S([O-])(=O)=O)S([O-])(=O)=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.
溶解性数据 for NF 023
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 100 |
制备储备液 for NF 023
以下数据基于产品分子量 1162.86。 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 | 0.86 mL | 4.3 mL | 8.6 mL |
| 5 mM | 0.17 mL | 0.86 mL | 1.72 mL |
| 10 mM | 0.09 mL | 0.43 mL | 0.86 mL |
| 50 mM | 0.02 mL | 0.09 mL | 0.17 mL |
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产品说明书 for NF 023
参考文献 for NF 023
参考文献是支持产品生物活性的出版物。
Freissmuth et al (1996) Suramin analogues as subtype-selective G protein inhibitors. Mol.Pharmacol. 49 602 PMID: 8609887
Sneddon et al (2000) The effect of P2 receptor antagonists and ATPase inhibition on sympathetic purinergic neurotransmission in the guinea-pig isolated vas deferens. Br.J.Pharmacol. 129 1089 PMID: 10725256
Soto et al (1999) Antagonistic properties of the suramin analogue NF023 at heterologously expressed P2X receptors. Neuropharmacology 38 141 PMID: 10193905
Van Rhee et al (1994) Novel competitive antagonists for P2 purinoceptors. Eur.J.Pharmacol. 268 1 PMID: 7925607
Su et al (2020) Identification of HMGA2 inhibitors by AlphaScreen-based ultra-high-throughput screening assays. Sci.Rep. 10 18850 PMID: 33139812
If you know of a relevant reference for NF 023, please let us know.
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关键词: NF 023, NF 023 supplier, inhibitors, inhibits, Go/i, α-subunits, alpha-subunits, P2X, purinoceptors, antagonists, Selective, competitive, G-Protein, Signaling, Signalling, Heterotrimeric, Receptors, Purinergic, NF023, HMGA2, high, mobility, group, protein, AT-hook, 2, DNA, bindin, G-protein, GTPases, 1240, Tocris Bioscience
10 篇 NF 023 的引用文献
引用文献是使用了 Tocris 产品的出版物。 NF 023 的部分引用包括：
Ren et al (2014) The approved pediatric drug suramin identified as a clinical candidate for the treatment of EV71 infection-suramin inhibits EV71 infection in vitro and in vivo. Emerg Microbes Infect 3 e62 PMID: 26038755
Su et al (2020) Identification of HMGA2 inhibitors by AlphaScreen-based ultra-high-throughput screening assays. Sci Rep 10 18850 PMID: 33139812
Nishimura et al (2015) The Suramin Derivative NF449 Interacts with the 5-fold Vertex of the Enterovirus A71 Capsid to Prevent Virus Attachment to PSGL-1 and Heparan Sulfate. PLoS Pathog 11 e1005184 PMID: 26430888
Beckham et al (2013) Acid ceramidase induces sphingosine kinase 1/S1P receptor 2-mediated activation of oncogenic Akt signaling. Oncogenesis 2 e49 PMID: 23732709
Donnelly-Roberts et al (2009) Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors. Br J Pharmacol 157 1203 PMID: 19558545
Manohar et al (2012) ATP release and autocrine signaling through P2X4 receptors regulate γδ T cell activation. J Leukoc Biol 92 787 PMID: 22753954
Ledderose et al (2016) Mitochondrial Dysfunction, Depleted Purinergic Signaling, and Defective T Cell Vigilance and Immune Defense. J Infect Dis 213 456 PMID: 26150546
Gao et al (2018) Research articleHemolysis in human erythrocytes by Clostridium perfringens epsilon toxin requires activation of P2 receptors. Virulence 9 1601 PMID: 30277122
Gallego et al (2008) Purinergic and nitrergic junction potential in the human colon. Am J Physiol Gastrointest Liver Physiol 295 G522 PMID: 18599588
Labrakakis et al (2003) Localization and function of ATP and GABAA receptors expressed by nociceptors and other postnatal sensory neurons in rat. J Physiol 549 131 PMID: 12665615
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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.