A 740003

Name: A 740003
Brand: Tocris Bioscience
SKU: 3701

Tocris Bioscience, part of Bio-Techne | Catalog # 3701

Citations (95)

COA / SDS

Potent and selective P2X7 antagonist

Key Product Details

Description:	Potent and selective P2X₇ antagonist
Chemical Name:	N-[1-[[(Cyanoamino)(5-quinolinylamino)methylene]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide
Purity:	≥97% (HPLC)
Molecular Weight:	474.55

View Full Technical Details for A 740003

Technical Data
Citations

Biological Activity for A 740003

A 740003 is a potent and selective P2X₇ receptor antagonist (IC₅₀ values are 18 and 40 nM for rat and human receptors respectively). Displays selectivity over a variety of P2X and P2Y receptors up to a concentration of 100 μM. Reduces nociception in animal models of persistent neuropathic and inflammatory pain. Also reduces neuroblastoma tumor growth in mice.

Compound Libraries for A 740003

A 740003 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for A 740003

M. Wt	474.55
Formula	C₂₆H₃₀N₆O₃
Storage	Store at +4°C
Purity	≥97% (HPLC)
CAS Number	861393-28-4
PubChem ID	11351968
InChi Key	PUHSRMSFDASMAE-UHFFFAOYSA-N
Smiles	CC(C)(C)C(NC(CC3=CC(OC)=C(OC)C=C3)=O)N/C(NC2=CC=CC1=NC=CC=C12)=N/C#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 740003

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	9.49	20

Preparing Stock Solutions for A 740003

The following data is based on the product molecular weight 474.55.

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
0.2 mM	10.54 mL	52.68 mL	105.36 mL
1 mM	2.11 mL	10.54 mL	21.07 mL
2 mM	1.05 mL	5.27 mL	10.54 mL
10 mM	0.21 mL	1.05 mL	2.11 mL

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References for A 740003

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

Amoroso The P2X7 receptor is a key modulator of the PI3K/GSK3β/VEGF signaling network: evidence in experimental neuroblastoma. Oncogene 2015 PMID: 25619831
King Novel P2X₇ receptor antagonists ease the pain. Br.J.Pharmacol. 2007 PMID: 17471176
Donnelly-Roberts Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors. Br.J.Pharmacol. 2009 PMID: 19558545
Honore A-740003 [N-(1-{[(cyanoimino)(5-quinolinylamino)methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective P2X₇ receptor antagonist, dose-dependently reduces neuropathic pain in the rat. J.Pharmacol.Exp.Ther. 2006 PMID: 16982702