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更新時(shí)間：2019-06-28

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產(chǎn)品活性：Darapladib 是一種有效的脂蛋白相關(guān)磷脂酶A2 (Lp-PLA2) 抑制劑，IC50 為 0.25 nM。

研究領(lǐng)域：metabolic Enzyme/Protease

作用靶點(diǎn)：Phospholipase

In Vitro: Mechanistic studies using steady state and transient kinetics indicate Darapladib (SB-480848) to be a freely reversible, non-covalently bound, inhibitor of rhLp-PLA2 with a Ki of 110 pM and an off-rate of 27 min. Potent inhibition of the enzyme in whole human plasma is confirmed (IC50=5 2 nM). Furthermore, the presence of Darapladib during the copper catalysed oxidation of human LDL prevents the production of lyso-PtdCho (IC50=4 3 nM) and subsequent monocyte chemotaxis (IC50=4 1 nM).

In Vivo: Additional in vivo studies with Darapladib indicated an oral bioavailability of 11 2% in the fed rat. The oral bioavailability of Darapladib is 28 4% in the dog. Furthermore excellent inhibition of Lp-PLA2 within the atherosclerotic plaque is achieved for Darapladib, with 95 1% inhibition observed 2 h after an oral dose of 30 mg/kg to the WHHL rabbit. Darapladib, a specific inhibitor of lipoprotein-associated phospholipase A2 (lp-PLA2), on inflammation and atherosclerotic formation in the low density lipoprotein receptor (LDLR)-deficient mice. the activity of serum lp-PLA2 is inhibited by more than 60% in LDLR-deficient mice after oral administration of 50 mg/kg once daily of Darapladib for 6 weeks. Darapladib significantly inhibits serum lp-PLA2 activity in LDLR-deficient mice.

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