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).
|Storage||Desiccate at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solubility||Soluble to 100 mM in water|
Preparing Stock Solutions
The following data is based on the product molecular weight 1162.86. Batch specific molecular weights may vary from batch to batch due to solvent 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|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
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
If you know of a relevant reference for NF 023, please let us know.
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Keywords: inhibitors inhibits Go/i α-subunits alpha-subunits P2X purinoceptors antagonists Selective competitive G-Protein Signaling Signalling Heterotrimeric Receptors Purinergic NF023 P2X Receptors
5 Citations for NF 023
Citations are publications that use Tocris products. Selected citations for NF 023 include:
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
Beckham et al (2013) Acid ceramidase induces sphingosine kinase 1/S1P receptor 2-mediated activation of oncogenic Akt signaling. Oncogenesis 2 e49 PMID: 23732709
Manohar et al (2012) ATP release and autocrine signaling through P2X4 receptors regulate γδ T cell activation. J Leukoc Biol 92 787 PMID: 22753954
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
Do you know of a great paper that uses NF 023 from Tocris? If so please let us know.
Literature in this Area
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.