SB-435495

SB-435495 is a potent, selective, reversible, non-covalent and orally active Lp-PLA 2 inhibitor with an IC 50 of 0.06 nM In Vitro SB-435495 inhibits CYP450 3A4 with an IC 50 of 10 μM and the black membrane permeability is 0.017 cm/h. SB-435495 (5 μM; 24 h) significantly inhibits the expression of Lp-PLA 2 protein, while increases the expression levels of AMPKα and phosphorylated-AMPKα (T172) in oxLDL-exposed HUVECs. SB-435495 (5 μM; 24-72 h) significantly increases cell viability and NO expression, significantly decreases ET-1 expression in the oxLDL-exposed HUVECs. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: oxLDL-exposed human umbilical vein endothelial cells Concentration: 5 μM Incubation Time: 24 h Result: The expression of Lp-PLA 2 protein was significantly inhibited. Increased the expression levels of AMPKα and phosphorylated-AMPKα (T172). Cell Viability AssayCell Line: oxLDL-exposed human umbilical vein endothelial cells Concentration: 5 μM Incubation Time: 24, 48 and 72 h Result: Significantly increased cell viability. In Vivo SB-435495 (10 mg/kg; p.o.; once) inhibits plasma Lp-PLA 2 in the WHHL rabbit . SB-435495 (10 mg/kg; i.p.; daily for 28 days) effectively suppresses blood–retinal barrier (BRB) breakdown in Streptozotocin -diabetic Brown Norway rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:Lp-PLA2 0.06 nM (IC 50 )

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