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Submit ReviewNF 157
说明： Selective P2Y11 and P2X1 antagonist
化学名： 8,8'-[Carbonylbis[imino-3,1-phenylenecarbonylimino(4-fluoro-3,1-phenylene)carbonylimino]]bis-1,3,5-naphthalenetrisulfonic acid hexasodium salt
纯度： ≥90% (HPLC)
生物活性 for NF 157
NF 157 is a purinergic receptor antagonist that potently inhibits P2Y11 receptor activity (IC50 = 463 nM). Displays selectivity for P2Y11 and P2X1 receptors over P2Y1, P2Y2, P2X2, P2X3, P2X4 and P2X7 receptors. Inhibits NAD+-induced activation of human granulocytes.
This product is supplied with a high degree of hydration and some residual NaCl, the amount of which are batch dependent. Please refer to the Certificate of Analysis to obtain the batch specific Net Product Content and the maximum solubility threshold to use in dilution calculations.
技术数据 for NF 157
| 分子量 | 1437.08 |
| 公式 | C49H28F2N6Na6O23S6 |
| 储存 | Desiccate at RT |
| 纯度 | ≥90% (HPLC) |
| CAS Number | 104869-26-3 |
| PubChem ID | 71433548 |
| InChI Key | QJFCMJZVZFAWGF-UHFFFAOYSA-H |
| Smiles | [Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[O-]OOSC1=C2C(NC(=O)C3=CC(NC(=O)C4=CC(NC(=O)NC5=CC(=CC=C5)C(=O)NC5=CC(=CC=C5F)C(=O)NC5=CC=C(C6=CC(=CC(=C56)S([O-])(=O)=O)S([O-])(=O)=O)S([O-])(=O)=O)=CC=C4)=C(F)C=C3)=CC=C(C2=CC(=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 157
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 5 | 4 | |
| DMSO | 10 | 7 |
制备储备液 for NF 157
以下数据基于产品分子量 1437.08。 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 |
|---|---|---|---|
| 0.07 mM | 9.94 mL | 49.7 mL | 99.41 mL |
| 0.35 mM | 1.99 mL | 9.94 mL | 19.88 mL |
| 0.7 mM | 0.99 mL | 4.97 mL | 9.94 mL |
| 3.5 mM | 0.2 mL | 0.99 mL | 1.99 mL |
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产品说明书 for NF 157
参考文献 for NF 157
参考文献是支持产品生物活性的出版物。
Ullmann et al (2005) Synthesis and structure-activity relationships of suramin-derived P2Y11 receptor antagonists with nanomolar potency. J.Med.Chem. 48 7040 PMID: 16250663
Moreschi et al (2006) Extracellular NAD+ is an agonist of the human P2Y11 purinergic receptor in human granulocytes. J.Biol.Chem. 281 31419 PMID: 16926152
If you know of a relevant reference for NF 157, please let us know.
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关键词: NF 157, NF 157 supplier, Selective, P2Y11/P2X1, antagonists, Receptors, Purinergic, purinoceptors, NF157, antagonises, inhibitors, inhibits, P2X, P2Y, 2450, Tocris Bioscience
12 篇 NF 157 的引用文献
引用文献是使用了 Tocris 产品的出版物。 NF 157 的部分引用包括：
Avanzato et al (2016) Activation of P2X7 and P2Y11 purinergic receptors inhibits migration and normalizes tumor-derived endothelial cells via cAMP signaling Scientific Reports 6 32602 PMID: 27586846
Ledderose et al (2016) Mitochondrial Dysfunction, Depleted Purinergic Signaling, and Defective T Cell Vigilance and Immune Defense. J Infect Dis 213 456 PMID: 26150546
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
Kinoshita et al (2018) Anti-Depressant Flu Reveals its Therapeutic Effect Via Astrocytes. EBioMedicine 32 72 PMID: 29887330
Kawano et al (2015) Autocrine Regulation of UVA-Induced IL-6 Production via Release of ATP and Activation of P2Y Receptors. PLoS One 10 e0127919 PMID: 26030257
Ohtomo et al (2011) Increase of intracellular Ca2+ by purinergic receptors in cultured rat lacrimal gland myoepithelial cells. Invest Ophthalmol Vis Sci 52 9503 PMID: 22039237
Dosch et al (2019) Connexin-43-dependent ATP release mediates macrophage activation during sepsis. Elife 8 PMID: 30735126
Braganhol et al (2015) Nucleotide receptors control IL-8/CXCL8 and MCP-1/CCL2 secretions as well as proliferation in human glioma cells. Biochim Biophys Acta 1852 120 PMID: 25445541
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
Talasila et al (2009) Characterization of P2Y receptor subtypes functionally expressed on neonatal rat cardiac myofibroblasts. Br J Pharmacol 158 339 PMID: 19422377
Wu et al (2019) Antagonism of P2Y11 receptor (P2Y11R) protects epidermal stem cells against UV-B irradiation. Am J Transl Res 11 4738 PMID: 31497195
Manohar et al (2012) ATP release and autocrine signaling through P2X4 receptors regulate γδ T cell activation. J Leukoc Biol 92 787 PMID: 22753954
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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.