A 839977

Pricing Availability   Qty
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)
Reviews
Literature (5)

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.

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 for A 839977

Certificate of Analysis / Product Datasheet
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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


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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


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Reviews for A 839977

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.