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Darapladib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:356057-34-6
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
达拉地
SB-480848
产品介绍
Darapladib 是脂蛋白相关磷脂酶A2 (Lp-PLA2) 抑制剂,IC50=0.25 nM。

产品描述

Darapladib(IC50=0.25 nM) is a substituted pyrimidone with inhibitory activity towards lipoprotein-associated phospholipase-A2 (Lp-PLA2).

体外活性

During the copper catalysed oxidation of human LDL, Darapladib prevents the production of lyso-PtdCho with IC50 of 4 nM and subsequent monocyte chemotaxis with IC50 of 4 nM. [1]

体内活性

In the WHHL rabbits, Darapladib (30 mg/kg p.o.) exhibits excellent inhibition of Lp-PLA2 within the atherosclerotic plaque by 95%. [1] Darapladib, as an inhibitor of Lp-PLA2, reduces development of advanced coronary atherosclerosis in diabetic and hypercholesterolemic (DMHC) pigs. [2] In DMHC pigs, darapladib reduces the amount of IgG-immunopositive material that leaked into the brain and also the density of Aβ42-containing neurons. [3]

Cas No.

356057-34-6

分子式

C36H38F4N4O2S

分子量

666.77

别名

达拉地;SB-480848

储存和溶解度

DMSO:93 mg/mL (139.5 mM)
Ethanol:93 mg/mL (139.5 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years