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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.
|Storage||Desiccate at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||1.39 mL||6.96 mL||13.92 mL|
|2.5 mM||0.28 mL||1.39 mL||2.78 mL|
|5 mM||0.14 mL||0.7 mL||1.39 mL|
|25 mM||0.03 mL||0.14 mL||0.28 mL|
References are publications that support the biological activity of the product.
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
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Keywords: NF 157, NF 157 supplier, Selective, P2Y11/P2X1, antagonists, Receptors, Purinergic, purinoceptors, NF157, P2X, P2Y, 2450, Tocris Bioscience
11 Citations for NF 157
Citations are publications that use Tocris products. Selected citations for NF 157 include:
Dosch et al (2019) Connexin-43-dependent ATP release mediates macrophage activation during sepsis. Elife 8 PMID: 30735126
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
Ledderose et al (2016) Mitochondrial Dysfunction, Depleted Purinergic Signaling, and Defective T Cell Vigilance and Immune Defense. J Infect Dis 213 456 PMID: 26150546
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
Manohar et al (2012) ATP release and autocrine signaling through P2X4 receptors regulate γδ T cell activation. J Leukoc Biol 92 787 PMID: 22753954
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
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
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Literature in this Area
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.