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.
|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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 1096.9. 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||0.91 mL||4.56 mL||9.12 mL|
|5 mM||0.18 mL||0.91 mL||1.82 mL|
|10 mM||0.09 mL||0.46 mL||0.91 mL|
|50 mM||0.02 mL||0.09 mL||0.18 mL|
References are publications that support the products' biological activity.
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) he 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
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Keywords: NF 110, supplier, Potent, P2X3, antagonists, Receptors, Purinergic, purinoceptors, NF110, P2X, Receptors, P2X, Receptors, Tocris Bioscience
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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.