AZ 11645373

Pricing Availability Delivery Time Qty
Cat.No. 3317 - AZ 11645373 | C24H21N3O5S | CAS No. 227088-94-0
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)
Datasheet
Citations (5)
Literature

Biological Activity

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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

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

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.16 mL 10.79 mL 21.57 mL
5 mM 0.43 mL 2.16 mL 4.31 mL
10 mM 0.22 mL 1.08 mL 2.16 mL
50 mM 0.04 mL 0.22 mL 0.43 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.

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 PMID:


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

5 Citations for AZ 11645373

Citations are publications that use Tocris products. Selected citations for AZ 11645373 include:

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

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


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