Biological Activity
Potent and selective human P2X7 antagonist (KB values are 5 - 7 and > 10,000 nM at hP2X7 and rP2X7 respectively) that is completely without effect at all other P2X subtypes. Inhibits BzATP-mediated calcium influx and inhibits ATP-mediated IL-1β release in vitro (KB values are 15 and 92 nM respectively).
Licensing Information
Sold for research purposes under agreement from AstraZeneca
Technical Data
| M. Wt | 463.51 |
| Formula | C24H21N3O5S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 227088-94-0 |
| PubChem ID | 9804433 |
| InChI Key | VQEHBLGYANQWEA-UHFFFAOYSA-N |
| Smiles | O=C(CSC4=O)N4C(COC2=CC=C(C3=CC=CC([N+]([O-])=O)=C3)C=C2)CCC1=CC=NC=C1 |
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 | |||
| DMSO | 4.64 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 463.51. 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 | 2.16 mL | 10.79 mL | 21.57 mL |
| 5 mM | 0.43 mL | 2.16 mL | 4.31 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.16 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Stokes et al (2006) Characterization of a selective and potent antagonist of human P2X7 receptors, AZ11645373. Br.J.Pharmacol. 149 880 PMID: 17031385
Michel et al (2009) Mechanism of action of species-selective P2X(7) receptor antagonists. Br.J.Pharmacol. 156 1312 PMID: 19309360
Alcaraz et al (2003) Novel P2X7 receptor antagonists. Bioorg.Med.Chem.Letts. 13 4043 PMID:
Keywords: AZ 11645373, supplier, Potent, selective, human, P2X7, antagonists, Receptors, Purinergic, purinoceptors, AZ11645373, AstraZeneca, P2X, Receptors, P2X, Receptors, Tocris Bioscience
