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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $44 | In Stock | |
2 mg | $64 | In Stock | |
5 mg | $97 | In Stock | |
10 mg | $172 | In Stock | |
25 mg | $347 | In Stock | |
50 mg | $563 | In Stock | |
100 mg | $786 | In Stock | |
500 mg | $1,590 | In Stock | |
1 mL x 10 mM (in DMSO) | $156 | In Stock |
Description | Darapladib (SB-480848)(IC50=0.25 nM) is a substituted pyrimidone with inhibitory activity towards lipoprotein-associated phospholipase-A2 (Lp-PLA2). |
Targets&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] |
Alias | SB-480848 |
Molecular Weight | 666.77 |
Formula | C36H38F4N4O2S |
Cas No. | 356057-34-6 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 45 mg/mL (67.49 mM) ![]() Ethanol: 93 mg/mL (139.5 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
Ethanol
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