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Biological Activity for NF 110
NF 110 is a high affinity P2X3 receptor antagonist (Ki values are 36, 82 and 4144 nM for P2X3, P2X1 and P2X2 recombinant receptors respectively). Shows no activity at P2Y1, P2Y2 and P2Y11 receptors (IC50 > 10 μM). Potently inhibits α,β-meATP-evoked desensitizing currents in rat DRG neurons (IC50 = 527 nM). Shows antitumor activity against several tumor types. Also inhibits DNA-binding activity of HMGA2 (IC50 = 0.87 μM).
Technical Data for NF 110
|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.
Solubility Data for NF 110
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for NF 110
The following data is based on the product molecular weight 1096.9. 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|
|0.4 mM||2.28 mL||11.4 mL||22.79 mL|
|2 mM||0.46 mL||2.28 mL||4.56 mL|
|4 mM||0.23 mL||1.14 mL||2.28 mL|
|20 mM||0.05 mL||0.23 mL||0.46 mL|
References for NF 110
References are publications that support the biological activity of the product.
Dhar et al (2000) Antitumour activity of suramin analogues in human tumour cell lines and primary cultures of tumour cells from patients. Eur.J.Cancer 36 803 PMID: 10762755
Kassack et al (2004) Structure-activity relationships of analogues of NF449 confirm NF449 as the most potent and selective known P2X1 receptor antagonist. Eur.J.Med.Chem. 39 345 PMID: 15072843
Hausmann et al (2006) The suramin analog 4,4',4'',4'''-(Carbonylbis(imino-5,1,3-benzenetriylbis (carbonylimino)))tetra-kis-benzenesulfonic acid (NF110) potently blocks P2X3 receptors: subtype selectivity is determined by location of sulfonic Mol.Pharmacol. 69 2058 PMID: 16551782
Su et al (2020) Identification of HMGA2 inhibitors by AlphaScreen-based ultra-high-throughput screening assays. Sci.Rep. 10 18850 PMID: 33139812
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4 Citations for NF 110
Citations are publications that use Tocris products. Selected citations for NF 110 include:
Su et al (2020) Identification of HMGA2 inhibitors by AlphaScreen-based ultra-high-throughput screening assays. Sci Rep 10 18850 PMID: 33139812
Dosch et al (2019) Connexin-43-dependent ATP release mediates macrophage activation during sepsis. Elife 8 PMID: 30735126
Chandra et al (2019) Decoy Receptor Interactions as Novel Drug Targets against EKC-Causing Human Adenovirus. Viruses 11 PMID: 30870979
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
Do you know of a great paper that uses NF 110 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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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.