| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| R422578-1ml |
1ml |
现货  |
|
| 英文别名 | (R)-N-(isoquinolin-1-yl)-3-(4-methoxyphenyl)-N-(piperidin-3-yl)propanamide | PF-00932239 |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | R-IMPP |
| 生化机理 | R-IMPP 是一种 PCSK9 分泌抑制剂，半数最大抑制浓度 [IC50] = 4.8 μM。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 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。 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 |
| ALogP | 3.684 |
|---|---|
| HBD Count | 1 |
| Rotatable Bond | 6 |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IIUPAC Name | N-isoquinolin-1-yl-3-(4-methoxyphenyl)-N-[(3R)-piperidin-3-yl]propanamide |
| INCHI | 1S/C24H27N3O2/c1-29-21-11-8-18(9-12-21)10-13-23(28)27(20-6-4-15-25-17-20)24-22-7-3-2-5-19(22)14-16-26-24/h2-3,5,7-9,11-12,14,16,20,25H,4,6,10,13,15,17H2,1H3/t20-/m1/s1 |
| InChi Key | OKTGXQMSOIQCTJ-HXUWFJFHSA-N |
| Smiles | COC1=CC=C(C=C1)CCC(=O)N(C2CCCNC2)C3=NC=CC4=CC=CC=C43 |
| Isomeric SMILES | COC1=CC=C(C=C1)CCC(=O)N([C@@H]2CCCNC2)C3=NC=CC4=CC=CC=C43 |
| PubChem CID | 122198706 |
| 分子量 | 389.49 |
| DMSO(mg / mL) Max Solubility | 77 |
|---|---|
| DMSO(mM) Max Solubility | 197.6944209 |
| Water(mg / mL) Max Solubility | 7 |
| Water(mM) Max Solubility | 17.97222008 |
| 分子量 | 389.500 g/mol |
| XLogP3 | 3.800 |
| 氢键供体数Hydrogen Bond Donor Count | 1 |
| 氢键受体数Hydrogen Bond Acceptor Count | 4 |
| 可旋转键计数Rotatable Bond Count | 6 |
| 精确质量Exact Mass | 389.21 Da |
| 单同位素质量Monoisotopic Mass | 389.21 Da |
| 拓扑极表面积Topological Polar Surface Area | 54.500 Ų |
| 重原子数Heavy Atom Count | 29 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 520.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 1 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| 象形图 | GHS07 |
|---|---|
| 信号词 | 警告 |
| 危险声明 |
H302: 吞食有害 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 |
| 预防措施声明 |
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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