A 804598

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Cat.No. 4473 - A 804598 | C19H17N5 | CAS No. 1125758-85-1
Description: Potent and selective P2X7 antagonist
Chemical Name: N-Cyano-N"-[(1S)-1-phenylethyl]-N'-5-quinolinyl-guanidine
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Literature

Biological Activity

Potent, competitive P2X7 receptor antagonist (IC50 values are 8.9, 9.9 and 10.9 nM for mouse, rat and human P2X7 receptors respectively). Selective for P2X7 receptors (IC50 > 5-10 μM for a wide array of cell surface receptors and ion channels). Binds with high affinity (Ki app = 2.4 nM for rat P2X7 receptors).

Compound Libraries

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Technical Data

M. Wt 315.37
Formula C19H17N5
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 1125758-85-1
PubChem ID 53325874
InChI Key PQYCRDPLPKGSME-AWEZNQCLSA-N
Smiles C[C@@H](C3=CC=CC=C3)NC(NC2=CC=CC1=NC=CC=C12)=NC#N

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 31.54 100

Preparing Stock Solutions

The following data is based on the product molecular weight 315.37. 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 3.17 mL 15.85 mL 31.71 mL
5 mM 0.63 mL 3.17 mL 6.34 mL
10 mM 0.32 mL 1.59 mL 3.17 mL
50 mM 0.06 mL 0.32 mL 0.63 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.

Donnelly-Roberts et al (2009) [3H]A-804598 ([3H]2-cyano-1-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine) is a novel, potent, and selective antagonist radioligand for P2X7 receptors. Neuropharmacology 56 223 PMID: 18602931

Able et al (2011) Receptor localization, native tissue binding and ex vivo occupancy for centrally penetrant P2X7 antagonists in the rat. Br.J.Pharmacol. 162 405 PMID: 20840537


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Keywords: A 804598, supplier, A804598, purinergic, receptors, P2X7, antagonists, inhibitors, inhibits, potent, selective, competitive, high, affinity, P2X, Receptors, P2X, Receptors, Tocris Bioscience

1 Citation for A 804598

Citations are publications that use Tocris products. Selected citations for A 804598 include:

Young et al (2015) A novel mechanism of autophagic cell death in dystrophic muscle regulated by P2RX7 receptor large-pore formation and HSP90. Cell Commun Signal 11 113 PMID: 25700737


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