A7231
AZ11645373
≥98% (HPLC), solid
别名:
3-[1-[[(3′-nitro[1,1′-biphenyl]-4-yl)oxy]methyl]-3-(4-pyridinyl)propyl]-2,4-thiazolidinedione
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.
signalword
Danger
hcodes
Hazard Classifications
Eye Dam. 1 - Skin Irrit. 2 - STOT SE 3
target_organs
Respiratory system
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
法规信息
新产品
此项目有
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
Acetylation of SUMO1 Alters Interactions with the SIMs of PML and Daxx in a Protein-Specific Manner.
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
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
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
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