AZ 11645373

Name: AZ 11645373
Brand: Tocris Bioscience
SKU: 3317

Tocris Bioscience a Bio-Techne Brand

Catalog # 3317

Citations (7)

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Key Product Details

Description:	Potent and selective human P2X₇ antagonist
Chemical Name:	3-[1-[[(3'-Nitro[1,1'-biphenyl]-4-yl)oxy]methyl]-3-(4-pyridinyl)propyl]-2,4-thiazolidinedione
Purity:	≥98% (HPLC)
Molecular Weight:	463.51

View Full Technical Details for AZ 11645373

Biological Activity for AZ 11645373

AZ 11645373 is a potent and selective human P2X₇ antagonist (K_B values are 5 - 7 and > 10,000 nM at hP2X₇ and rP2X₇ respectively) that is completely without effect at all other P2X subtypes. Inhibits BzATP-mediated calcium influx and inhibits ATP-mediated IL-1β release in vitro (K_B values are 15 and 92 nM respectively).

Licensing Information

Sold for research purposes under agreement from AstraZeneca

Technical Data for AZ 11645373

M. Wt	463.51
Formula	C₂₄H₂₁N₃O₅S
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	227088-94-0
PubChem ID	9804433
InChi Key	VQEHBLGYANQWEA-UHFFFAOYSA-N
Smiles	O=C(CSC4=O)N4C(COC2=CC=C(C3=CC=CC([N+]([O-])=O)=C3)C=C2)CCC1=CC=NC=C1

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 AZ 11645373

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	4.64	10

Preparing Stock Solutions for AZ 11645373

The following data is based on the product molecular weight 463.51.

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
0.1 mM	21.57 mL	107.87 mL	215.75 mL
0.5 mM	4.31 mL	21.57 mL	43.15 mL
1 mM	2.16 mL	10.79 mL	21.57 mL
5 mM	0.43 mL	2.16 mL	4.31 mL

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References for AZ 11645373

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

Michel Mechanism of action of species-selective P2X(7) receptor antagonists. Br.J.Pharmacol. 2009 PMID: 19309360
Stokes Characterization of a selective and potent antagonist of human P2X₇ receptors, AZ11645373. Br.J.Pharmacol. 2006 PMID: 17031385
Alcaraz Novel P2X₇ receptor antagonists. Bioorg.Med.Chem.Letts.

Citations for AZ 11645373 (7)

Showing 1 - 7 of 7 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for AZ 11645373 include:

Karmakar et al. (2016) Neutrophil P2X₇ receptors mediate NLRP3 inflammasome-dependent IL-1β secretion in response to ATP. Nat.Commun.. 7:10555
PMID: 26877061
Agrawal et al. (2016) P2X₇Rs are involved in cell death, growth and cellular signaling in primary human osteoblasts Bone. 95:91
PMID: 27856358
Kawano et al. (2015) Autocrine Regulation of UVA-Induced IL-6 Production via Release of ATP and Activation of P2Y Receptors. PLoS One. 10:e0127919
PMID: 26030257
Soares-Bezerra et al. (2015) An Improved Method for P2X7R Antagonist Screening. Arthritis Rheumatol. 10:e0123089
PMID: 25993132
Sathanoori et al. (2015) The ATP Receptors P2X7 and P2X4 Modulate High Glucose and Palmitate-Induced Inflammatory Responses in Endothelial Cells. PLoS One. 10:e0125111
PMID: 25938443
Bhaskaracharya et al. (2014) Probenecid blocks human P2X7 receptor-induced dye uptake via a pannexin-1 independent mechanism. PLoS One. 9:e93058
PMID: 24671093
Foster et al. (2013) Mitochondrial superoxide generation enhances P2X7R-mediated loss of cell surface CD62L on naive human CD4+ T lymphocytes. J Immunol. 190:1551
PMID: 23319734

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Showing 1 - 7 of 7 citations Showing All

Product Documents for AZ 11645373

COA

Certificate of Analysis

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