A 839977

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Cat.No. 4232 - A 839977 | C19H14Cl2N6O | CAS No. 870061-27-1
Description: Potent P2X7 antagonist
Chemical Name: 1-(2,3-Dichlorophenyl)-N-[[2-(2-pyridinyloxy)phenyl]methyl]-1H-tetrazol-5-amine
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Literature

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

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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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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


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Keywords: A 839977, supplier, A839977, purinergics, purinoceptors, purines, p2x7, antagonists, antinociceptive, cns, penetrant, P2X, Receptors, P2X, Receptors, 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


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Pathways for A 839977

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