Biological Activity
Potent P2X7 antagonist; blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20, 42 and 150 nM respectively). Displays antinociceptive effects in rat and mice models of inflammatory pain. CNS penetrant.
Compound Libraries
A 839977 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 413.26 |
| Formula | C19H14Cl2N6O |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 870061-27-1 |
| PubChem ID | 53325875 |
| InChI Key | GMVNBKZQJFRFAR-UHFFFAOYSA-N |
| Smiles | ClC(C(Cl)=CC=C4)=C4N1N=NN=C1NCC2=CC=CC=C2OC3=NC=CC=C3 |
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 | 41.33 | 100 | |
| ethanol | 2.07 | 5 |
Preparing Stock Solutions
The following data is based on the product molecular weight 413.26. 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 | 2.42 mL | 12.1 mL | 24.2 mL |
| 5 mM | 0.48 mL | 2.42 mL | 4.84 mL |
| 10 mM | 0.24 mL | 1.21 mL | 2.42 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Honore et al (2009) The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1αβ knockout mice. Behav.Brain.Res. 204 77 PMID: 19464323
Friedle et al (2010) Recent patents on novel P2X7 receptor antagonists and their potential for reducing central nervous system inflammation. Recent Pat.CNS Drug Discov. 5 35 PMID: 19705995
Keywords: A 839977, supplier, A839977, purinergics, purinoceptors, purines, p2x7, antagonists, antinociceptive, cns, penetrant, P2X, Receptors, P2X, Receptors, Tocris Bioscience
