NF 449

Cat. No. 1391

NF 449 C41H24N6Na8O29S8 [627034-85-9]

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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.

Certificate of Analysis / Safety Data Sheet

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Fleming et al (2011) Chemical modulators of autophagy as biological probes and potential therapeutics. Nat.Chem.Biol. 7 9. PMID: 21164513.

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-benzene-1,3-disulfonic acid octasodium salt]. J.Pharmacol.Exp.Ther. 314 232. PMID: 15792995.

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.

Hohenegger et al (1998) G-selective G protein antagonists. Proc.Natl.Acad.Sci.U.S.A. 95 346. PMID: 9419378.

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Citations are publications that use Tocris products. Selected citations for NF 449 include:

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.

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.

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.

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.

Ibáñez et al (2012) A high throughput scintillation proximity imaging assay for protein methyltransferases. Comb Chem High Throughput Screen 15 359. PMID: 22256970.

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.

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.

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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Keywords: NF 449, supplier, selective, P2X1, antagonists, Receptors, Purinergic, purinoceptors, NF449, Tocris Bioscience, Purinergic (P2X) Receptor Antagonist products

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