A-484954CAS号: 142557-61-7分子式: C13H15N5O3分子量: 289.29描述纯度储存/保存方法别名外观可溶性/溶解性In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
A-484954 is a highly selective eukaryotic elongationfactor-2 (eEF2) inhibitor, with an IC50 of 280 nM.
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纯度 |
98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
A484954
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外观 |
white to beige powder
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可溶性/溶解性 |
DMSO : 20 mg/mL (69.13 mM; Need ultrasonic)
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生物活性 | |
In vitro(体外研究) |
A-484954 is a highly selective eEF2K inhibitor with an IC50 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 IC50 value of A-484954 is increased as the concentration of ATP increased but unaffected by increasing concentrations of calmodulin.
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In vivo(体内研究) |
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.
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分子结构图