Biological Activity
A subtype-selective, competitive and reversible P2X1 receptor antagonist. Displays IC50 values of 0.21, 28.9, > 50 and > 100 μM for human P2X1, P2X3, P2X2, and P2X4-mediated responses respectively. Selective over adrenoceptors, histamine and P2Y receptors. Also selectively inhibits the α-subunit of Go/i (EC50 ~300 nM).
Technical Data
| M. Wt | 1162.86 |
| Formula | C35H20N4Na6O21S6 |
| Storage | Desiccate at RT |
| CAS Number | 104869-31-0 |
| PubChem ID | 4465 |
| InChI Key | FMQURVHYTBGYSQ-UHFFFAOYSA-H |
| Smiles | [Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[O-]S(=O)(=O)C1=CC2=C(C=CC(NC(=O)C3=CC=CC(NC(=O)NC4=CC(=CC=C4)C(=O)NC4=C5C(C=C(C=C5S([O-])(=O)=O)S([O-])(=O)=O)=C(C=C4)S([O-])(=O)=O)=C3)=C2C(=C1)S([O-])(=O)=O)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
| Solubility | Soluble to 100 mM in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 1162.86. 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 | 0.86 mL | 4.3 mL | 8.6 mL |
| 5 mM | 0.17 mL | 0.86 mL | 1.72 mL |
| 10 mM | 0.09 mL | 0.43 mL | 0.86 mL |
| 50 mM | 0.02 mL | 0.09 mL | 0.17 mL |
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References
References are publications that support the products' biological activity.
Freissmuth et al (1996) Suramin analogues as subtype-selective G protein inhibitors. Mol.Pharmacol. 49 602 PMID: 8609887
Sneddon et al (2000) The effect of P2 receptor antagonists and ATPase inhibition on sympathetic purinergic neurotransmission in the guinea-pig isolated vas deferens. Br.J.Pharmacol. 129 1089 PMID: 10725256
Soto et al (1999) Antagonistic properties of the suramin analogue NF023 at heterologously expressed P2X receptors. Neuropharmacology 38 141 PMID: 10193905
Van Rhee et al (1994) Novel competitive antagonists for P2 purinoceptors. Eur.J.Pharmacol. 268 1 PMID: 7925607
Keywords: NF 023, supplier, inhibitors, inhibits, Go/i, α-subunits, alpha-subunits, P2X, purinoceptors, antagonists, Selective, competitive, G-Protein, Signaling, Signalling, Heterotrimeric, Receptors, Purinergic, NF023, P2X, Receptors, G, Protein, (Heterotrimeric), P2X, Receptors, Tocris Bioscience
