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Category: Ion ChannelsarrowLigand-gated Ion ChannelsarrowP2X ReceptorsarrowAntagonists
Cat.No. Product Name
1391 NF 449
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NF 449
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 anti-thrombotic protection in vivo. Also acts as a Gsα-selective antagonist.

Technical Data:

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M.Wt: 1505.06
Formula: C41H24N6Na8O29S8
Storage: Store at RT
Solubility: Soluble to 50 mM in Water
CAS No: [389142-38-5]

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    References:

    Hohenegger et al (1998) Gσα-selective G protein antagonists. Proc.Natl.Acad.Sci. 95 346. 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. 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.
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    Keywords: NF 449, Ligand-gated Ion Channels, Highly Selective P2X1 Antagonist, NF449, Tocris Bioscience
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