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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).
|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|
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
References are publications that support the biological activity of the product.
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.
Keywords: 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
Citations are publications that use Tocris products. Selected citations for NF 023 include:
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
Gao et al (2018) Research articleHemolysis in human erythrocytes by Clostridium perfringens epsilon toxin requires activation of P2 receptors. Virulence 9 1601 PMID: 30277122
Ledderose et al (2016) Mitochondrial Dysfunction, Depleted Purinergic Signaling, and Defective T Cell Vigilance and Immune Defense. J Infect Dis 213 456 PMID: 26150546
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
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
Manohar et al (2012) ATP release and autocrine signaling through P2X4 receptors regulate γδ T cell activation. J Leukoc Biol 92 787 PMID: 22753954
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
Gallego et al (2008) Purinergic and nitrergic junction potential in the human colon. Am J Physiol Gastrointest Liver Physiol 295 G522 PMID: 18599588
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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.