Catalog Number: 1391
Chemical Name: 4,4',4'',4'''-[Carbonylbis(imino-5,1,3-benzenetriyl-bis(carbonylimino))]tetrakis-1,3-benzenedisulfonic acid, octasodium salt
Biological Activity
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.
Technical Data
  • M.Wt:
    1505.06
  • Formula:
    C41H24N6Na8O29S8
  • Solubility:
    Soluble to 50 mM in water with gentle warming
  • Storage:
    Store at RT
  • CAS No:
    627034-85-9
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.
Background References
  1. 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
    Hechler et al.
    J.Pharmacol.Exp.Ther., 2005;314:232
  2. G-selective G protein antagonists.
    Hohenegger et al.
    Proc.Natl.Acad.Sci.U.S.A., 1998;95:346
  3. Profiling at recombinant homomeric and heteromeric rat P2X receptors identifies the suramin analogue NF449 as a highly potent P2X1 receptor antagonist.
    Rettinger et al.
    Neuropharmacology., 2005;48:461
  4. Chemical modulators of autophagy as biological probes and potential therapeutics.
    Fleming et al.
    Nat.Chem.Biol., 2011;7:9
Citations:

The citations listed below are publications that use Tocris products. Selected citations for NF 449 include:

12 Citations: Showing 1 - 10
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  1. Optodynamic simulation of β-adrenergic receptor signalling.
    Authors: Siuda Et al.
    Purinergic Signal 2015;6:8480
  2. Effects of NAD at purine receptors in isolated blood vessels.
    Authors: Alefishat Et al.
    Circulation 2015;11:47
  3. 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.
    Authors: Ren Et al.
    Emerg Microbes Infect 2014;3:e62
  4. The G protein α subunit Gαs is a tumor suppressor in Sonic hedgehog-driven medulloblastoma.
    Authors: He Et al.
    Nat Med 2014;20:1035
  5. Development of high throughput screening assays and pilot screen for inhibitors of metalloproteases meprin α and β.
    Authors: Madoux Et al.
    Biopolymers 2014;102:396
  6. Pharmacological characterization of the P2 receptors profile in the podocytes of the freshly isolated rat glomeruli.
    Authors: Ilatovskaya Et al.
    Am J Physiol Cell Physiol 2013;305:C1050
  7. Long-term heart transplant survival by targeting the ionotropic purinergic receptor P2X7.
    Authors: Vergani Et al.
    Integr Biol (Camb) 2013;127:463
  8. A high throughput scintillation proximity imaging assay for protein methyltransferases.
    Authors: Ibáñez Et al.
    Comb Chem High Throughput Screen 2012;15:359
  9. Leucine deprivation stimulates fat loss via increasing CRH expression in the hypothalamus and activating the sympathetic nervous system.
    Authors: Cheng Et al.
    Mol Endocrinol 2011;25:1624
  10. P2Y12 or P2Y1 inhibitors reduce platelet deposition in a microfluidic model of thrombosis while apyrase lacks efficacy under flow conditions.
    Authors: Maloney Et al.
    Lipids Health Dis 2010;2:183
  11. Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.
    Authors: Donnelly-Roberts Et al.
    Br J Pharmacol 2009;157:1203
  12. Identification of atropine- and P2X1 receptor antagonist-resistant, neurogenic contractions of the urinary bladder.
    Authors: Kennedy Et al.
    J Neurosci 2007;27:845
Expand to show all 12 Citations

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