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
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R-IMPP
Dangerous GoodsCAS number：2133832-83-2 molecular formula：C24H27N3O2
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | (R)-N-(isoquinolin-1-yl)-3-(4-methoxyphenyl)-N-(piperidin-3-yl)propanamide | PF-00932239 | ||
| CAS number | 2133832-83-2 | molecular formula | C24H27N3O2 |
| molecular weight | 389.49 g/mol | Exact mass | 10mM in DMSO |
| PSA | 54.500 Ų | logp | 3.684 |
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physicochemical properties
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害
Statement of Preventive Measures：
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
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