A-484954
A-484954 性质
| 沸点 | 522.9±60.0 °C(Predicted) |
|---|---|
| 密度 | 1.522±0.06 g/cm3 (20 ºC 760 Torr) |
| 储存条件 | 2-8°C |
| 溶解度 | DMSO：可溶，3mg/mL，澄清（加热） |
| 酸度系数(pKa) | 14.26±0.20(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| InChI | 1S/C13H15N5O3/c1-2-17-12(20)8-5-7(10(15)19)9(14)16-11(8)18(13(17)21)6-3-4-6/h5-6H,2-4H2,1H3,(H2,14,16)(H2,15,19) |
| InChIKey | HWODCHXORCTEGU-UHFFFAOYSA-N |
A-484954 用途与合成方法
IC50: 280 nM (eEF2).
A-484954 is a highly selective eEF2K inhibitor with an IC 50 value of 280 nM against eEF2K in the enzymatic assay and little activity against a wide panel of serine/threonine and tyrosine kinases. In enzymatic assay, the IC 50 value of A-484954 is increased as the concentration of ATP increased but unaffected by increasing concentrations of calmodulin.
A484954 causes relaxation in E (+) and E (-) aorta or mesenteric artery precontracted with NA. Pretreatment with L-NAME but not indomethacin or cimetidine partially inhibits the A484954-induced relaxation in mesenteric artery. Long-term A-484954 treatment inhibits MCT-induced increases PA pressure. It is revealed that A-484954 inhibits MCT-induced PA hypertrophy and fibrosis but not impairment of endothelium-dependent and -independent relaxation. Furthermore, A-484954 inhibits MCT-induced NADPH oxidase-1 expression and ROS generation as well as matrix metalloproteinase-2 activation.
安全信息
| 危险品标志 | T |
|---|---|
| 危险类别码 | 25-36/37/38 |
| 安全说明 | 26-45 |
| 危险品运输编号 | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
| 存储类别 | 6.1C - 可燃，急性毒性 类别3 毒性化合物或者引起慢性影响的化合物 |
A-484954 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025-12-22 | HY-110096 | 142557-61-7 | 1 mg | 380 | |
| 2025-12-22 | HY-110096 | A-484954 | 142557-61-7 | 5mg | 1000 |
