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