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检测方案
≥97.5% (HPLC)
形式
powder
储存条件
under inert gas
颜色
white
mp
133-135 °C
溶解性
DMSO: 20 mg/mL, clear
储存温度
2-8°C
SMILES字符串
OC(=O)CC[C@@H](Cc1ccc(OCc2ccccc2)cc1)NC(=O)CCCCCCc3ccccc3
InChI
1S/C31H37NO4/c33-30(16-10-2-1-5-11-25-12-6-3-7-13-25)32-28(19-22-31(34)35)23-26-17-20-29(21-18-26)36-24-27-14-8-4-9-15-27/h3-4,6-9,12-15,17-18,20-21,28H,1-2,5,10-11,16,19,22-24H2,(H,32,33)(H,34,35)/t28-/m0/s1
InChI key
KWLUIYFCMHKLKY-NDEPHWFRSA-N
应用
sPLA2抑制剂已被用于研究对于肺癌细胞和少突胶质细胞增殖和凋亡的影响。
分泌型磷脂酶A2抑制剂已用于：
- 人肺腺癌细胞的Matrigel侵袭实验
- 预处理培养的少突胶质细胞
- 抑制肺腺癌的分泌型磷脂酶A2。
生化/生理作用
sPLA2抑制剂（pla2g2a）是一种具有口服活性、有效的分泌型磷脂酶A2（sPLA2；组IIa）抑制剂。分泌型磷脂酶A2抑制剂可阻断NF-KB、Akt、p38 MAPK以及ERK通路的激活。sPLA2抑制剂可减少肺癌细胞的增殖并诱导其凋亡，是一种有效的抗炎剂。sPLA2抑制剂可防止胶原沉积，并在高血压大鼠中具有抗纤维化作用。
分泌型磷脂酶A2(sPLA2)抑制剂是分子量为487.63 Da的亲脂性分子。它调节炎症反应和脂蛋白功能，可用于治疗动脉粥样硬化。
分泌型磷脂酶A2抑制剂可阻断NF-κB、Akt、p38 MAPK以及ERK通路的激活。 它可减少肺癌细胞的增殖并诱导其凋亡，是一种有效的抗炎剂。 sPLA2抑制剂可防止胶原沉积，并在高血压大鼠中具有抗纤维化作用。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
法规信息
新产品
Alison L Halpern et al.
Digestive diseases and sciences, 66(3), 784-795 (2020-04-12)
Receptor tyrosine kinases of the epidermal growth factor receptor (EGFR) family such as human epidermal receptor-2 (HER2) are involved in the development and progression of esophageal adenocarcinoma (EAC). Prior studies have demonstrated that group IIa secretory phospholipase A2 (sPLA2 IIa)
Discovery of AZD2716: a novel secreted phospholipase A2 (sPLA2) inhibitor for the treatment of coronary artery disease
Giordanetto F, et al.
ACS Medicinal Chemistry Letters, 7(10), 884-889 (2016)
Robert C Reid
Current medicinal chemistry, 12(25), 3011-3026 (2005-12-28)
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 proven to exacerbate numerous diseases that have an inflammatory component. Current therapies include NSAIDs' that
Maung-Maung Thwin et al.
Arthritis research & therapy, 11(5), R138-R138 (2009-09-22)
Secretory phospholipase A2 (sPLA2) and matrix metalloproteinase (MMP) inhibitors are potent modulators of inflammation with therapeutic potential, but have limited efficacy in rheumatoid arthritis (RA). The objective of this study was to understand the inhibitory mechanism of phospholipase inhibitor from
Jessica A Yu et al.
Anticancer research, 32(9), 3601-3607 (2012-09-21)
Group IIa secretory phospholipase A2 (sPLA2 IIa) has been implicated in the regulation of metastasis of non-small cell lung cancer (NSCLC) and the present study investigates its contribution to lung cancer growth and progression. PLA2s initiate signaling in several pathways
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