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Submit ReviewA 839977
Description: Potent P2X7 antagonist
Chemical Name: 1-(2,3-Dichlorophenyl)-N-[[2-(2-pyridinyloxy)phenyl]methyl]-1H-tetrazol-5-amine
Purity: ≥98% (HPLC)
Biological Activity for A 839977
A 839977 is a 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.
Technical Data for A 839977
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for A 839977
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.33 | 100 |
Preparing Stock Solutions for A 839977
The following data is based on the product molecular weight 413.26. 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 | 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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References for A 839977
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for A 839977, please let us know.
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Keywords: A 839977, A 839977 supplier, A839977, purinergics, purinoceptors, purines, p2x7, antagonists, antinociceptive, cns, penetrant, P2X, Receptors, 4232, Tocris Bioscience
1 Citation for A 839977
Citations are publications that use Tocris products. Selected citations for A 839977 include:
Gangadharan et al (2015) Caveolin-1 regulates P2X7 receptor signaling in osteoblasts. PLoS One 308 C41 PMID: 25318104
Do you know of a great paper that uses A 839977 from Tocris? Please let us know.
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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