A-484954
作者：齊岳
發(fā)布時間：2023-09-12
08:53:03
點擊數(shù)：
產(chǎn)品名稱：A-484954
產(chǎn)品描述：
| 產(chǎn)品描述 | A 484954 is a highly specific eukaryotic elongation factor-2 (eEF2, IC50: 280 nM) inhibitor. |
| 靶點活性 | eEF2:280 nM |
| 體外活性 | A-484954 is a selective eEF2K inhibitor and little activity against a wide panel of serine/threonine and tyrosine kinases. In the enzymatic assay, the IC50 value of A-484954 is increased as the concentration of ATP increased but unaffected by increasing concentrations of calmodulin [1]. |
| 體內(nèi)活性 | Long-term A-484954 treatment inhibits MCT-induced increases PA pressure. Furthermore, A-484954 inhibits MCT-induced NADPH oxidase-1 expression and ROS generation as well as matrix metalloproteinase-2 activation [2]. 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 [3]. |
| 別名 | A 484954 |
| 分子量 | 289.29 |
| 分子式 | C13H15N5O3 |
| CAS No. | 142557-61-7 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: Insoluble
DMSO: 20 mg/mL (69.13 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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