Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Darapladib (SB-480848)(IC50=0.25 nM) is a substituted pyrimidone with inhibitory activity towards lipoprotein-associated phospholipase-A2 (Lp-PLA2).
説明 | Darapladib (SB-480848)(IC50=0.25 nM) is a substituted pyrimidone with inhibitory activity towards lipoprotein-associated phospholipase-A2 (Lp-PLA2). |
ターゲット&IC50 | Lp-PLA2:0.25 nM |
In vitro | 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] |
In vivo | 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] |
別名 | SB-480848 |
分子量 | 666.77 |
分子式 | C36H38F4N4O2S |
CAS No. | 356057-34-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 45 mg/mL (67.49 mM)
Ethanol: 93 mg/mL (139.5 mM)
You can also refer to dose conversion for different animals. 詳細
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Darapladib 356057-34-6 Metabolism Phospholipase SB 480848 inhibit Inhibitor SB480848 SB-480848 inhibitor