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3-{1-[(3'-硝基-4-联苯基)氧基]-4-(4-吡啶基)-2-丁烷基}-1,3-噻唑烷-2,4-二酮

用途

AZ11645373是一种对人而非大鼠P2X7受体具有高度选择性和强效的拮抗剂,AZ116453 73抑制脂多糖激活的THP-1细胞释放ATP诱导的IL-1β,IC50值为90 nM[1]。

名称

[ CAS 号 ]:
227088-94-0

[ 中文名 ]:
3-{1-[(3'-硝基-4-联苯基)氧基]-4-(4-吡啶基)-2-丁烷基}-1,3-噻唑烷-2,4-二酮

[ 英文名 ]:
AZ 11645373

[英文别名 ]:

unii-xy4szp4c72

生物活性

[ 描述 ]:

AZ11645373是一种对人而非大鼠P2X7受体具有高度选择性和强效的拮抗剂,AZ116453 73抑制脂多糖激活的THP-1细胞释放ATP诱导的IL-1β,IC50值为90 nM[1]。

[ 相关类别 ]:

研究领域 >> 炎症/免疫

信号通路 >> 跨膜转运 >> P2X受体

[体外研究]

AZ11645373对 BzATP公司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纳米的浓度下观察到完全抑制[1] AZ11645373在稳定表达 hP2X7R基因的赫克细胞中抑制三磷酸腺苷或 BzATP公司诱发的约-1荧光,但在表达 rP2X7R型的细胞中没有抑制作用,千字节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、1μM；30分钟) 对脂多糖处理细胞培养基中 IL-1β的基础水平没有显著影响,但对三磷酸腺苷介导的 IL-1β释放产生浓度依赖性抑制,计算出的千字节值为 92纳米[1]

[参考文献]

[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.

物理化学性质

[ 分子式 ]:
C₂₄H₂₁N₃O₅S

[ 分子量 ]:
463.51

[ 精确质量 ]:
463.12000

[ PSA ]:
130.62000

[ LogP ]:
5.19350

[ 储存条件 ]:
2-8°C，干燥，密封

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 符号 ]:

GHS05, GHS07

[ 信号词 ]:
Danger

[ 危害声明 ]:
H315-H318-H335

[ 警示性声明 ]:
P261-P280-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
37/38-41

[ 安全声明 (欧洲) ]:
26-39

[ 危险品运输编码 ]:
NONH for all modes of transport

文献

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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