AZ 11645373

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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)
Citations (7)
Literature (5)

Biological Activity for AZ 11645373

AZ 11645373 is a potent and selective human P2X7 antagonist (KB 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 (KB 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
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 Data for AZ 11645373

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets for AZ 11645373

Certificate of Analysis / Product Datasheet
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References for AZ 11645373

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

Stokes et al (2006) Characterization of a selective and potent antagonist of human P2X7 receptors, AZ11645373. Br.J.Pharmacol. 149 880 PMID: 17031385

Michel et al (2009) Mechanism of action of species-selective P2X(7) receptor antagonists. Br.J.Pharmacol. 156 1312 PMID: 19309360

Alcaraz et al (2003) Novel P2X7 receptor antagonists. Bioorg.Med.Chem.Letts. 13 4043

If you know of a relevant reference for AZ 11645373, please let us know.

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Keywords: AZ 11645373, AZ 11645373 supplier, Potent, selective, human, P2X7, antagonists, Receptors, Purinergic, purinoceptors, AZ11645373, AstraZeneca, P2X, 3317, Tocris Bioscience

7 Citations for AZ 11645373

Citations are publications that use Tocris 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

Soares-Bezerra et al (2015) An Improved Method for P2X7R Antagonist Screening. Arthritis Rheumatol 10 e0123089 PMID: 25993132

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

Do you know of a great paper that uses AZ 11645373 from Tocris? Please let us know.

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Literature in this Area

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