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。 Information R-IMPP R-IMPP is an inhibitor of PCSK9 secretion, half maximal inhibitory concentration [IC50] = 4.8 μM. Targets PCSK9 In vitro R-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