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Darapladib

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Chemical Structure| 356057-34-6 同义名 : 达拉地 ;SB-480848
CAS号 : 356057-34-6
货号 : A684359
分子式 : C36H38F4N4O2S
纯度 : 99%+
分子量 : 666.771
MDL号 : MFCD18251452
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(157.48 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Darapladib is a potent Lp-PLA2 (lipoprotein-associated phospholipase A2) inhibitor with IC50 value of 0.25nM. Treatment of DMHC (diabetes mellitus and hypercholesterolemia) animals with darapladib reduced the amount of IgG-immunopositive material that leaked into the brain as well as the density of Aβ42-containing neurons, suggesting the reduction of blood–brain barrier permeability by darapladib. Treatment with darapladib blocked atherosclerosis progression and improves animal alertness and activity levels in a porcine DMHC model.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.50mL

0.30mL

0.15mL

7.50mL

1.50mL

0.75mL

15.00mL

3.00mL

1.50mL
参考文献

[1]Blackie JA, Bloomer JC, et al. The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2. Bioorg Med Chem Lett. 2003 Mar 24;13(6):1067-70.

[2]Acharya NK, Levin EC, et al. Diabetes and hypercholesterolemia increase blood-brain barrier permeability and brain amyloid deposition: beneficial effects of the LpPLA2 inhibitor darapladib. J Alzheimers Dis. 2013;35(1):179-98.