NF 449

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Cat.No. 1391 - NF 449 | C41H24N6Na8O29S8 | CAS No. 627034-85-9
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
Datasheet
Citations (12)
Literature

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
Storage Store at RT
CAS Number 627034-85-9
PubChem ID 91895233
InChI Key PHCBPKWKKHYRSA-UHFFFAOYSA-F
Smiles [Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[O-]S(=O)(=O)C1=CC=C(NC(=O)C2=CC(=CC(NC(=O)NC3=CC(=CC(=C3)C(=O)NC3=CC=C(C=C3S([O-])(=O)=O)S([O-])(=O)=O)C(=O)NC3=CC=C(C=C3S([O-])(=O)=O)S([O-])(=O)=O)=C2)C(=O)NC2=CC=C(C=C2S([O-])(=O)=O)S([O-])(=O)=O)C(=C1)S([O-])(=O)=O

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 75.26 50mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 1505.06. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.66 mL 3.32 mL 6.64 mL
5 mM 0.13 mL 0.66 mL 1.33 mL
10 mM 0.07 mL 0.33 mL 0.66 mL
50 mM 0.01 mL 0.07 mL 0.13 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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) G-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


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Keywords: NF 449, supplier, selective, P2X1, antagonists, Receptors, Purinergic, purinoceptors, NF449, P2X, Receptors, Autophagy, P2X, Receptors, Tocris Bioscience

12 Citations for NF 449

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

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

Vergani et al (2013) Long-term heart transplant survival by targeting the ionotropic purinergic receptor P2X7. Integr Biol (Camb) 127 463 PMID: 23250993

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

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

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

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

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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