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Merck
CN

A7231

AZ11645373

≥98% (HPLC), solid

Synonym(s):

3-[1-[[(3′-nitro[1,1′-biphenyl]-4-yl)oxy]methyl]-3-(4-pyridinyl)propyl]-2,4-thiazolidinedione

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About This Item

Empirical Formula (Hill Notation):
C24H21N3O5S
CAS Number:
227088-94-0
Molecular Weight:
463.51
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid

Key Documents

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InChI

1S/C24H21N3O5S/c28-23-16-33-24(29)26(23)21(7-4-17-10-12-25-13-11-17)15-32-22-8-5-18(6-9-22)19-2-1-3-20(14-19)27(30)31/h1-3,5-6,8-14,21H,4,7,15-16H2

InChI key

VQEHBLGYANQWEA-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

solid

color

tan

solubility

DMSO: ≥10 mg/mL

originator

AstraZeneca

storage temp.

2-8°C

Application

AZ11645373 is a selective and potent human P2X7 purinoceptor antagonist. AZ11645373 has been used in the rhesus macaque monkey to elucidate the mechanisms and pharmacological interventions of P2X7 receptor-related diseases.

Biochem/physiol Actions

AZ11645373 is a selective and potent human P2X7 purinoceptor antagonist. KB values range from 5-20 nM for human P2X7 receptor inhibition. It is 500-fold less effective ats an inhibitor of rat P2X7 receptor responses.
Selective and potent human P2X7 purinoceptor antagonist

Features and Benefits

This compound is featured on the P2 Receptors: P2X Ion Channel Family page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by AstraZeneca. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

pictograms

CorrosionExclamation mark
GHS05,GHS07

signalword

Danger

Hazard Classifications

Eye Dam. 1 - Skin Irrit. 2 - STOT SE 3

target_organs

Respiratory system

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

dust mask type N95 (US), Eyeshields, Gloves

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
117K46122
117K46121
117K4612

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Xavier H Mascle et al.
Structure (London, England : 1993), 28(2), 157-168 (2019-12-28)
The interactions between SUMO proteins and SUMO-interacting motif (SIM) in nuclear bodies formed by the promyelocytic leukemia (PML) protein (PML-NBs) have been shown to be modulated by either phosphorylation of the SIMs or acetylation of SUMO proteins. However, little is
L Stokes et al.
British journal of pharmacology, 149(7), 880-887 (2006-10-13)
The ATP-gated P2X(7) receptor has been shown to play a role in several inflammatory processes, making it an attractive target for anti-inflammatory drug discovery. We have recently identified a novel set of cyclic imide compounds that inhibited P2X(7) receptor-mediated dye
K Wareham et al.
British journal of pharmacology, 157(7), 1215-1224 (2009-06-26)
P2X receptors are widely expressed in cells of the immune system with varying functions. This study sought to characterize P2X receptor expression in the LAD2 human mast cell line and human lung mast cells (HLMCs). Reverse transcriptase polymerase chain reaction
Gloria Lopez-Castejon et al.
Journal of immunology (Baltimore, Md. : 1950), 185(4), 2611-2619 (2010-07-20)
The ATP-gated P2X(7) receptor (P2X(7)R) is a promising therapeutic target in chronic inflammatory diseases with highly specific antagonists currently under clinical trials for rheumatoid arthritis. Anti-inflammatory actions of P2X(7)R antagonists are considered to result from inhibition of P2X(7)R-induced release of
Helen J Bradley et al.
British journal of pharmacology, 164(2b), 743-754 (2011-04-05)
The human P2X7 (hP2X7) receptor exhibits striking pharmacological differences from its rodent counterparts, particularly in terms of its antagonist profile. Here, we characterized the functional and pharmacological properties of the rhesus macaque monkey P2X7 (rmP2X7) receptor in comparison with the

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