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Biological Activity for NF 449
NF 449 is a potent purinergic receptor antagonist that displays high selectivity for P2X1 (IC50 values are 0.28, 0.69, 120, 1820, 47000 and > 300000 nM for rP2X1, rP2X1+5, rP2X2+3, rP2X3, rP2X2 and P2X4 receptors respectively). Provides antithrombotic protection in vivo. Also acts as a Gsα-selective antagonist. Also inhibits DNA-binding activity of HMGA2 (IC50 = 0.43 μM).
Technical Data for NF 449
|Storage||Store 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 449
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|water||75.26||50 with gentle warming|
Preparing Stock Solutions for NF 449
The following data is based on the product molecular weight 1505.06. 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|
|0.5 mM||1.33 mL||6.64 mL||13.29 mL|
|2.5 mM||0.27 mL||1.33 mL||2.66 mL|
|5 mM||0.13 mL||0.66 mL||1.33 mL|
|25 mM||0.03 mL||0.13 mL||0.27 mL|
References for NF 449
References are publications that support the biological activity of the product.
Hechler et al (2005) Inhibition of platelet functions and thrombosis through selective or non-selective inhibition of the platelet P2 receptors with increasing doses of NF449 [4,4',4",4'"-(carbonylbis(imino-5,1,3-benzenetriylbis-(carbonylimino)))tetrakis-benze J.Pharmacol.Exp.Ther. 314 232 PMID: 15792995
Hohenegger et al (1998) Gsα-selective G protein antagonists. Proc.Natl.Acad.Sci.U.S.A. 95 346 PMID: 9419378
Rettinger et al (2005) Profiling at recombinant homomeric and heteromeric rat P2X receptors identifies the suramin analogue NF449 as a highly potent P2X1 receptor antagonist. Neuropharmacology. 48 461 PMID: 15721178
Fleming et al (2011) Chemical modulators of autophagy as biological probes and potential therapeutics. Nat.Chem.Biol. 7 9 PMID: 21164513
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 449, please let us know.
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21 Citations for NF 449
Citations are publications that use Tocris products. Selected citations for NF 449 include:
Su et al (2020) Identification of HMGA2 inhibitors by AlphaScreen-based ultra-high-throughput screening assays. Sci Rep 10 18850 PMID: 33139812
Johansson et al (2019) Shiga toxin signals via ATP and its effect is blocked by purinergic receptor antagonism. Sci.Rep. 9 14362 PMID: 31591425
Li et al (2017) Follicular Stimulating Hormone Accelerates Atherogenesis by Increasing Endothelial VCAM-1 Expression. Theranostics 7 4671 PMID: 29187895
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
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
Fresco et al (2004) Facilitation of noradrenaline release by activation of adenosine A(2A) receptors triggers both phospholipase C and adenylate cyclase pathways in rat tail artery. Cardiovasc Res 63 739 PMID: 15306230
Ilatovskaya et al (2013) Pharmacological characterization of the P2 receptors profile in the podocytes of the freshly isolated rat glomeruli. Am J Physiol Cell Physiol 305 C1050 PMID: 24048730
Cheng et al (2011) Leucine deprivation stimulates fat loss via increasing CRH expression in the hypothalamus and activating the sympathetic nervous system. Mol Endocrinol 25 1624 PMID: 21719534
Chandra et al (2019) Decoy Receptor Interactions as Novel Drug Targets against EKC-Causing Human Adenovirus. Viruses 11 PMID: 30870979
Madoux et al (2014) Development of high throughput screening assays and pilot screen for inhibitors of metalloproteases meprin α and β. Biopolymers 102 396 PMID: 25048711
He et al (2014) The G protein α subunit Gαs is a tumor suppressor in Sonic hedgehog-driven medulloblastoma. Nat Med 20 1035 PMID: 25150496
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
Vergani et al (2013) Long-term heart transplant survival by targeting the ionotropic purinergic receptor P2X7. Integr Biol (Camb) 127 463 PMID: 23250993
Kennedy et al (2007) Identification of atropine- and P2X1 receptor antagonist-resistant, neurogenic contractions of the urinary bladder. J Neurosci 27 845 PMID: 17251425
Zhang et al (2018) Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility. Elife 7 PMID: 29393851
Gao et al (2018) Research articleHemolysis in human erythrocytes by Clostridium perfringens epsilon toxin requires activation of P2 receptors. Virulence 9 1601 PMID: 30277122
Maloney et al (2010) P2Y12 or P2Y1 inhibitors reduce platelet deposition in a microfluidic model of thrombosis while apyrase lacks efficacy under flow conditions. Lipids Health Dis 2 183 PMID: 20473398
Palygin et al (2018) Characterization of purinergic receptor expression in ARPKD cystic epithelia. Purinergic Signal 14 485 PMID: 30417216
Siuda et al (2015) Optodynamic simulation of β-adrenergic receptor signalling. Purinergic Signal 6 8480 PMID: 26412387
Alefishat et al (2015) Effects of NAD at purine receptors in isolated blood vessels. Circulation 11 47 PMID: 25315718
Ibáñez et al (2012) A high throughput scintillation proximity imaging assay for protein methyltransferases. Comb Chem High Throughput Screen 15 359 PMID: 22256970
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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.