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GSK2647544

更新时间:2025-08-31 17:12:41

GSK2647544结构式
GSK2647544结构式
品牌特惠专场
常用名 GSK2647544 英文名 GSK2647544
CAS号 1380426-95-8 分子量 502.87
密度 N/A 沸点 N/A
分子式 C24H18ClF3N4O3 熔点 N/A
MSDS N/A 闪点 N/A

 GSK2647544用途


GSK2647544是一种口服的选择性Lp-PLA2抑制剂。脂蛋白相关磷脂酶(Lp-PLA2)是一种钙非依赖性磷脂酶A2,具有促炎活性,主要由单核细胞衍生的巨噬细胞分泌[1]。

 GSK2647544名称

英文名 GSK2647544

 GSK2647544生物活性

描述 GSK2647544是一种口服的选择性Lp-PLA2抑制剂。脂蛋白相关磷脂酶(Lp-PLA2)是一种钙非依赖性磷脂酶A2,具有促炎活性,主要由单核细胞衍生的巨噬细胞分泌[1]。
相关类别
参考文献

[1]. Wu K, et al. Evaluation of the safety, pharmacokinetics, pharmacodynamics, and drug-drug interaction potential of a selective Lp-PLA2 inhibitor (GSK2647544) in healthy volunteers
. Int J Clin Pharmacol Ther. 2016;54(12):935-949.

 GSK2647544物理化学性质

分子式 C24H18ClF3N4O3
分子量 502.87
InChIKey DRACNSAQZFZUKW-UHFFFAOYSA-N
SMILES O=c1[nH]c(OCCc2ccc(Oc3ccc(Cl)c(C(F)(F)F)c3)cc2)ncc1Cc1cncnc1
外观性状 固体
储存条件 2-8°C, 避光

 GSK2647544靶点实验

查看更多实验

实验名称:Metabolic stability in human liver S9 fractions assessed as intrinsic clearance at 0....
来源:ChEMBL
靶标:Liver
External Id:CHEMBL3635128
实验名称:Inhibition of recombinant human Lp-PLA2 at 10 nM using 2-thio-PAF substrate after 10 ...
来源:ChEMBL
靶标:Platelet-activating factor acetylhydrolase
External Id:CHEMBL3635127
实验名称:Terminal half life in Sprague-Dawley rat at 25 mg/kg, po after 48 hrs by LC-MS method
来源:ChEMBL
靶标:Rattus norvegicus
External Id:CHEMBL3635255
实验名称:AUC (0 to infinity) in Sprague-Dawley rat at 25 mg/kg, po after 48 hrs by LC-MS metho...
来源:ChEMBL
靶标:Rattus norvegicus
External Id:CHEMBL3635129
实验名称:In vivo inhibition of Lp-PLA2 in mouse plasma at 100 nM after 24 hrs
来源:ChEMBL
靶标:Platelet-activating factor acetylhydrolase
External Id:CHEMBL3635116
实验名称:Metabolic stability in human liver S9 fractions assessed as half life at 0.1 uM in pr...
来源:ChEMBL
靶标:Liver
External Id:CHEMBL3635114
实验名称:Metabolic stability in Wistar rat liver S9 fractions assessed as half life at 0.1 uM ...
来源:ChEMBL
靶标:Liver
External Id:CHEMBL3635113
实验名称:Inhibition of Lp-PLA2 in human plasma at 10 nM using 2-thio-PAF substrate after 10 mi...
来源:ChEMBL
靶标:Platelet-activating factor acetylhydrolase
External Id:CHEMBL3635120
实验名称:Inhibition of Lp-PLA2 in Sprague-Dawley rat plasma at 100 nM using 2-thio-PAF substra...
来源:ChEMBL
靶标:N/A
External Id:CHEMBL3635119
实验名称:Inhibition of Lp-PLA2 in mouse plasma at 1 uM using 2-thio-PAF substrate after 10 min...
来源:ChEMBL
靶标:Platelet-activating factor acetylhydrolase
External Id:CHEMBL3635117
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