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sPLA2 inhibitor 1

sPLA2 inhibitor 1用途

sPLA2抑制剂1是一种D-酪氨酸衍生物,是一种口服有效的分泌型磷脂酶A2(sPLA2)抑制剂,对人非胰腺分泌型PLA2亚型IIa(HNPPLA2 IIa)的IC50为29 nM。sPLA2抑制剂1具有抗炎活性[1]。

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sPLA2 inhibitor 1名称

[ CAS 号 ]:
393569-31-8

[ 中文名 ]:
sPLA2抑制剂

[ 英文名 ]:
sPLA2 inhibitor 1

[英文别名 ]:

KH064
MFCD06411576
sPLA2 inhibitor

sPLA2 inhibitor 1生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 磷脂

研究领域 >> 炎症/免疫

[ 靶点 ]

sPLA2:29 nM (IC50)

[体内研究]

sPLA2抑制剂1(化合物2b；口服；5 mg/kg/天；接种关节炎原后第10-13天)显示出对水肿的显著抑制。药物治疗的大鼠表现为轻度囊性水肿和少量巨噬细胞浸润红髓[1]。

[参考文献]

[1]. Karl A Hansford, et al. D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity. Chembiochem. 2003 Mar 3;4(2-3):181-5.

sPLA2 inhibitor 1物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
720.9±60.0 °C at 760 mmHg

[ 分子式 ]:
C₃₁H₃₇NO₄

[ 分子量 ]:
487.63

[ 闪点 ]:
389.8±32.9 °C

[ 精确质量 ]:
487.272247

[ LogP ]:
6.16

[ 蒸汽压 ]:
0.0±2.4 mmHg at 25°C

[ 折射率 ]:
1.573

[ 储存条件 ]:
2-8°C

sPLA2 inhibitor 1安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
22-24/25

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

sPLA2 inhibitor 1文献

Inhibitors of secretory phospholipase A2 group IIA.

Curr. Med. Chem. 12(25) , 3011-26, (2005)

Phospholipases A2 cleave membrane phospholipids to release arachidonic acid, the precursor to a large family of pro-inflammatory eicosanoids including prostaglandins and leukotrienes that have been pr...

Antifibrotic activity of an inhibitor of group IIA secretory phospholipase A2 in young spontaneously hypertensive rats.

J. Immunol. 176(11) , 7000-7, (2006)

The development of fibrosis in the chronically hypertensive heart is associated with infiltration of inflammatory cells and cardiac hypertrophy. In this study, an inhibitor of the proinflammatory enzy...

Group IIa secretory phospholipase expression correlates with group IIa secretory phospholipase inhibition-mediated cell death in K-ras mutant lung cancer cells.

J. Thorac. Cardiovasc. Surg. 144(6) , 1479-85, (2012)

There are currently no targeted therapies against lung tumors with oncogenic K-ras mutations that are found in 25% to -40% of lung cancers and are characterized by their resistance to epidermal growth...

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