A 804598

Name: A 804598
Brand: Tocris Bioscience
SKU: 4473
Rating: 5 (1 reviews)

Tocris Bioscience a Bio-Techne Brand

Catalog # 4473

Citations (2)

(1)

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Key Product Details

Description:	Potent and selective P2X₇ antagonist
Chemical Name:	N-Cyano-N"-[(1S)-1-phenylethyl]-N'-5-quinolinyl-guanidine
Purity:	≥99% (HPLC)
Molecular Weight:	315.37

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Biological Activity for A 804598

A 804598 is a 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 (K_{i app} = 2.4 nM for rat P2X₇ receptors).

Compound Libraries for A 804598

A 804598 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for A 804598

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for A 804598

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	31.54	100

Preparing Stock Solutions for A 804598

The following data is based on the product molecular weight 315.37.

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	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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References for A 804598

References are publications that support the biological activity of the product.

Able Receptor localization, native tissue binding and ex vivo occupancy for centrally penetrant P2X7 antagonists in the rat. Br.J.Pharmacol. 2011 PMID: 20840537
Donnelly-Roberts [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 2009 PMID: 18602931

Citations for A 804598 (2)

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Citations are publications that use Bio-Techne products. Selected citations for A 804598 include:

Dosch et al. (2019) Connexin-43-dependent ATP release mediates macrophage activation during sepsis. Elife. 8
PMID: 30735126
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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A 804598 inhibits LPS-induced inflammation

Name: Anonymous

Species: Mouse

Assay Type: In Vitro

Cell Line/Tissue: Macrophages

RAW macrophages were stimulated with LPS (200 ng/ml) in the absence or presence of A 804598 (1 μM) or MRS 2578 (100 μM) for 8 h to follow iNOS expression by qPCR. Both compounds inhibited LPS-induced iNOS expression revealing role of purinergic receptors.

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Product Documents for A 804598

COA

Certificate of Analysis

To download a Certificate of Analysis, please select a batch below.