AZ 11645373

Pricing Availability   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 (7)
Reviews
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.

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

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
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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Certificate of Analysis / Product Datasheet
Select another batch:

References

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.

View Related Products by Target

View Related Products by Product Action

View all Purinergic (P2X) Receptor Antagonists

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:

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

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

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

Agrawal et al (2016) P2X7Rs are involved in cell death, growth and cellular signaling in primary human osteoblasts Bone 95 91 PMID: 27856358

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.

Reviews for AZ 11645373

There are currently no reviews for this product. Be the first to review AZ 11645373 and earn rewards!

Have you used AZ 11645373?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cardiovascular

Cardiovascular Research Product Guide

A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

  • Hypertension
  • Thrombosis and Hemostasis
  • Atherosclerosis
  • Myocardial Infarction
  • Ischemia/Reperfusion Injury
  • Arrhythmias
  • Heart Failure
Ion Channel

Ion Channel Product Listing

A collection of around 500 products for ion channel research, the listing includes research tools for the study of:

  • Ligand-gated ion channels
  • Voltage-gated ion channels
  • Other Ion Channels
Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling
P2X and P2Y Receptors

P2X and P2Y Receptors Scientific Review

Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.

Pain

Pain Poster

Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.