AZ 11645373

[Description]:

AZ11645373 is a highly selective and potent antagonist at human but not rat P2X7 receptors，AZ11645373 inhibits ATP-evoked IL-1β release from lipopolysaccharide-activated THP-1 cells , with an IC50 value of 90 nM[1].

[Related Catalog]:

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Membrane Transporter/Ion Channel >> P2X Receptor

[In Vitro]

AZ11645373 对 BzATP 介导的钙瞬变产生浓度依赖性抑制，根据浓度抑制曲线，在 100 至 300 nM 的浓度下观察到完全抑制[1]。 AZ11645373 在稳定表达 hP2X7R 的 HEK 细胞中抑制 ATP 或 BzATP 诱发的 YO-PRO1 荧光，但在表达 rP2X7R 的细胞中没有抑制作用，KB 值与测量膜电流或钙动员的实验中获得的值没有显著差异[1]。 AZ11645373 (0.01、0.1、1 μM；30 分钟) 对 LPS 处理细胞培养基中 IL-1β 的基础水平没有显著影响，但对 ATP 介导的 IL-1β 释放产生浓度依赖性抑制，计算出的 KB 值为 92 nM[1]。

[References]

[1]. Stokes L, et al. Characterization of a selective and potent antagonist of human P2X(7) receptors, AZ11645373. Br J Pharmacol. 2006 Dec;149(7):880-7.

[ Molecular Formula ]:
C₂₄H₂₁N₃O₅S

[ Molecular Weight ]:
463.51

[ Exact Mass ]:
463.12000

[ PSA ]:
130.62000

[ LogP ]:
5.19350

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[ Symbol ]:

GHS05, GHS07

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H315-H318-H335

[ Precautionary Statements ]:
P261-P280-P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xi: Irritant;

[ Risk Phrases ]:
37/38-41

[ Safety Phrases ]:
26-39

[ RIDADR ]:
NONH for all modes of transport

Characterization of a selective and potent antagonist of human P2X(7) receptors, AZ11645373.

Br. J. Pharmacol. 149 , 880-887, (2006)

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 ...

Functional evidence for the expression of P2X1, P2X4 and P2X7 receptors in human lung mast cells.

Br. J. Pharmacol. 157 , 1215-24, (2009)

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 ...

P2X(7) receptor-mediated release of cathepsins from macrophages is a cytokine-independent mechanism potentially involved in joint diseases.

J. Immunol. 185 , 2611-9, (2010)

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. An...

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