| 产品描述: | PCSK9 抑制剂;PCSK9 Inhibitors;产品介绍:R-IMPP (PF-00932239) 是一种 PCSK9 的抗分泌药物 (IC50=4.8 μM),其靶向 80S 核糖体抑制 PCSK9 蛋白翻译。;InformationR-IMPP R-IMPP is an inhibitor of PCSK9 secretion, half maximal inhibitory concentration [IC50] = 4.8 μM.TargetsPCSK9In vitroR-IMPP promotes uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin. R-IMPP does not decrease PCSK9 transcription or increase PCSK9 degradation, but instead causes transcript-dependent inhibition of PCSK9 translation. R-IMPP is discovered that exhibited weak PCSK9 anti-secretagogue activity (half maximal inhibitory concentration [IC50] = 4.8 μM), but does not affect intracellular ATP levels in the recombinant CHO-K1 cells, a measure of cytotoxicity, nor decrease secretion of a control protein, secreted alkaline phosphatase, a measure of relative selectivity. The inhibitory response of R-IMPP is stereospecific.Cell Research(from reference)Cell lines:Huh7 cells Concentrations:10, 30 μM Incubation Time:24 h |