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NF 279 is a a potent and selective P2X1 antagonist (IC50 = 19 nM). Displays good selectivity over P2X2,(IC50 = 0.76 μM), P2X3 (IC50 = 1.62μM), P2X4 (IC50 > 300 μM), P2Y receptors and ecto-nucleotidases.
This product is supplied with a high degree of hydration and some residual NaCl, the amount of which are batch dependent. Please refer to the Certificate of Analysis to obtain the batch specific Net Product Content.
|Storage||Store at -20°C|
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 1401.1. 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|
|0.18 mM||3.97 mL||19.83 mL||39.65 mL|
|0.9 mM||0.79 mL||3.97 mL||7.93 mL|
|1.8 mM||0.4 mL||1.98 mL||3.97 mL|
|9 mM||0.08 mL||0.4 mL||0.79 mL|
References are publications that support the biological activity of the product.
Damer et al (1998) NF279: a novel potent and selective antagonist of P2X receptor-mediated responses. Eur.J.Pharmacol. 350 R5 PMID: 9683026
Klapperstuck et al (2000) Antagonism by the suramin analogue NF 279 on human P2X1 and P2X7 receptors. Eur.J.Pharmacol. 387 245 PMID: 10650169
Rettinger et al (2000) The suramin analogue NF279 is a novel and potent antagonist selective for the P2X1 receptor. Neuropharmacology 39 2044 PMID: 10963748
If you know of a relevant reference for NF 279, please let us know.
Keywords: NF 279, NF 279 supplier, Potent, selective, P2X1, antagonists, Receptors, Purinergic, purinoceptors, NF279, P2X, 1199, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for NF 279 include:
Ibáñez et al (2012) A high throughput scintillation proximity imaging assay for protein methyltransferases. Comb Chem High Throughput Screen 15 359 PMID: 22256970
Hazleton et al (2012) Purinergic receptors are required for HIV-1 infection of primary human macrophages. J Immunol 188 4488 PMID: 22450808
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
Inscho et al (2003) Physiological role for P2X1 receptors in renal microvascular autoregulatory behavior. J Clin Invest 112 1895 PMID: 14679185
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
Aliagas et al (2014) High expression of ecto-nucleotidases CD39 and CD73 in human endometrial tumors. PLoS One 2014 509027 PMID: 24707115
Aliagas et al (2013) Reduced striatal ecto-nucleotidase activity in schizophrenia patients supports the "adenosine hypothesis". Purinergic Signal 9 599 PMID: 23771238
Luke and Hexum (2008) UTP and ATP increase extracellular signal-regulated kinase 1/2 phosphorylation in bovine chromaffin cells through epidermal growth factor receptor transactivation. Mediators Inflamm 4 323 PMID: 18777108
Kennedy et al (2007) Identification of atropine- and P2X1 receptor antagonist-resistant, neurogenic contractions of the urinary bladder. J Neurosci 27 845 PMID: 17251425
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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.