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NF 449

Catalog #: 1391
21 Citations Datasheet
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1391/50
NF 449 | CAS No. 627034-85-9 | P2X Receptor Antagonists
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Description: Highly selective P2X1 antagonist

Chemical Name: 4,4',4'',4'''-[Carbonylbis(imino-5,1,3-benzenetriyl-bis(carbonylimino))]tetrakis-1,3-benzenedisulfonic acid, octasodium salt

Purity: ≥90%

Product Details
Citations (21)
Supplemental Products
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

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).

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 and the maximum solubility threshold to use in dilution calculations.

Technical Data

M.Wt:
1505.06
Formula:
C41H24N6Na8O29S8
Solubility:
Soluble to 25 mg/ml in water
Purity:
≥90%
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Gq activity- and ?-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility
    DL Zhang, YJ Sun, ML Ma, YJ Wang, H Lin, RR Li, ZL Liang, Y Gao, Z Yang, DF He, A Lin, H Mo, YJ Lu, MJ Li, W Kong, KY Chung, F Yi, JY Li, YY Qin, J Li, ARB Thomsen, AW Kahsai, ZJ Chen, ZG Xu, M Liu, D Li, X Yu, JP Sun
    Elife, 2018;7(0):.
  2. Role of Purinergic Receptor Expression and Function for Reduced Responsiveness to Adenosine Diphosphate in Washed Human Platelets.
    Koessler J, Hermann S, Weber K, Koessler A, Kuhn S, Boeck M, Kobsar A
    PLoS ONE, 2016;11(1):e0147370.
  3. Molecular signaling underlying bulleyaconitine A (BAA)-induced microglial expression of prodynorphin
    TF Li, HY Wu, YR Wang, XY Li, YX Wang
    Sci Rep, 2017;7(0):45056.
  4. The role of adenosine diphosphate mediated platelet responsiveness for the stability of platelet integrity in citrated whole blood under ex vivo conditions
    J Koessler, M Schwarz, K Weber, J Etzel, A Koessler, M Boeck, A Kobsar
    PLoS ONE, 2017;12(11):e0188193.
  5. Overexpression of CD39 in mouse airways promotes bacteria-induced inflammation.

    J. Immunol., 2012;189(4):1966-74.
  6. Chemical modulators of autophagy as biological probes and potential therapeutics.
    Fleming et al.
    Nat.Chem.Biol., 2011;7:9
  7. Gsα-selective G protein antagonists.
    Hohenegger et al.
    Proc.Natl.Acad.Sci.U.S.A., 1998;95:346
  8. 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
  9. 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
  10. Identification of HMGA2 inhibitors by AlphaScreen-based ultra-high-throughput screening assays.
    Su et al.
    Sci.Rep., 2020;10:18850

Product Datasheets

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Citations for NF 449

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

21 Citations: Showing 1 - 10

  1. Identification of HMGA2 inhibitors by AlphaScreen-based ultra-high-throughput screening assays.
    Authors: Su Et al.
    Sci Rep  2020;10:18850
  2. Shiga toxin signals via ATP and its effect is blocked by purinergic receptor antagonism.
    Authors: Johansson Et al.
    Sci.Rep.  2019;9:14362
  3. Decoy Receptor Interactions as Novel Drug Targets against EKC-Causing Human Adenovirus.
    Authors: Chandra Et al.
    Viruses  2019;11
  4. Research articleHemolysis in human erythrocytes by Clostridium perfringens epsilon toxin requires activation of P2 receptors.
    Authors: Gao Et al.
    Virulence  2018;9:1601
  5. Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility.
    Authors: Zhang Et al.
    Elife  2018;7
  6. Characterization of purinergic receptor expression in ARPKD cystic epithelia.
    Authors: Palygin Et al.
    Purinergic Signal  2018;14:485
  7. Follicular Stimulating Hormone Accelerates Atherogenesis by Increasing Endothelial VCAM-1 Expression.
    Authors: Li Et al.
    Theranostics  2017;7:4671
  8. Optodynamic simulation of β-adrenergic receptor signalling.
    Authors: Siuda Et al.
    Purinergic Signal  2015;6:8480
  9. 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.
    Authors: Nishimura Et al.
    PLoS Pathog  2015;11:e1005184
  10. Effects of NAD at purine receptors in isolated blood vessels.
    Authors: Alefishat Et al.
    Circulation  2015;11:47
  11. 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
  12. The G protein α subunit Gαs is a tumor suppressor in Sonic hedgehog-driven medulloblastoma.
    Authors: He Et al.
    Nat Med  2014;20:1035
  13. 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
  14. 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
  15. Long-term heart transplant survival by targeting the ionotropic purinergic receptor P2X7.
    Authors: Vergani Et al.
    Integr Biol (Camb)  2013;127:463
  16. A high throughput scintillation proximity imaging assay for protein methyltransferases.
    Authors: Ibáñez Et al.
    Comb Chem High Throughput Screen  2012;15:359
  17. 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
  18. 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
  19. Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.
    Authors: Donnelly-Roberts Et al.
    Br J Pharmacol  2009;157:1203
  20. Identification of atropine- and P2X1 receptor antagonist-resistant, neurogenic contractions of the urinary bladder.
    Authors: Kennedy Et al.
    J Neurosci  2007;27:845
  21. Facilitation of noradrenaline release by activation of adenosine A(2A) receptors triggers both phospholipase C and adenylate cyclase pathways in rat tail artery.
    Authors: Fresco Et al.
    Cardiovasc Res  2004;63:739

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