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Submit ReviewA 804598
Description: Potent and selective P2X7 antagonist
Chemical Name: N-Cyano-N"-[(1S)-1-phenylethyl]-N'-5-quinolinyl-guanidine
Purity: ≥99% (HPLC)
Biological Activity
Potent, competitive P2X7 receptor antagonist (IC50 values are 8.9, 9.9 and 10.9 nM for mouse, rat and human P2X7 receptors respectively). Selective for P2X7 receptors (IC50 > 5-10 μM for a wide array of cell surface receptors and ion channels). Binds with high affinity (Ki app = 2.4 nM for rat P2X7 receptors).
Compound Libraries
A 804598 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 315.37 |
| Formula | C19H17N5 |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1125758-85-1 |
| PubChem ID | 53325874 |
| InChI Key | PQYCRDPLPKGSME-AWEZNQCLSA-N |
| Smiles | C[C@@H](C3=CC=CC=C3)NC(NC2=CC=CC1=NC=CC=C12)=NC#N |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 31.54 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 315.37. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 3.17 mL | 15.85 mL | 31.71 mL |
| 5 mM | 0.63 mL | 3.17 mL | 6.34 mL |
| 10 mM | 0.32 mL | 1.59 mL | 3.17 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.63 mL |
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References
References are publications that support the biological activity of the product.
Donnelly-Roberts et al (2009) [3H]A-804598 ([3H]2-cyano-1-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine) is a novel, potent, and selective antagonist radioligand for P2X7 receptors. Neuropharmacology 56 223 PMID: 18602931
Able et al (2011) Receptor localization, native tissue binding and ex vivo occupancy for centrally penetrant P2X7 antagonists in the rat. Br.J.Pharmacol. 162 405 PMID: 20840537
If you know of a relevant reference for A 804598, please let us know.
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Keywords: A 804598, A 804598 supplier, A804598, purinergic, receptors, P2X7, antagonists, inhibitors, inhibits, potent, selective, competitive, high, affinity, P2X, Receptors, 4473, Tocris Bioscience
2 Citations for A 804598
Citations are publications that use Tocris products. Selected citations for A 804598 include:
Dosch et al (2019) Connexin-43-dependent ATP release mediates macrophage activation during sepsis. Elife 8 PMID: 30735126
Young et al (2015) A novel mechanism of autophagic cell death in dystrophic muscle regulated by P2RX7 receptor large-pore formation and HSP90. Cell Commun Signal 11 113 PMID: 25700737
Do you know of a great paper that uses A 804598 from Tocris? Please let us know.
Reviews for A 804598
Average Rating: 5 (Based on 1 Review.)
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A 804598 inhibits LPS-induced inflammation.
By
Anonymous on 01/22/2019
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Macrophages
RAW macrophages were stimulated with LPS (200 ng/ml) in the absence or presence of A 804598 (1 μM) or MRS 2578 (100 μM) for 8 h to follow iNOS expression by qPCR. Both compounds inhibited LPS-induced iNOS expression revealing role of purinergic receptors.
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