A-484954
| 中文名称 | A-484954 |
|---|---|
| 中文同义词 | 7-氨基-1-环丙基-3-乙基-1,2,3,4-四氢-2,4-二氧代-吡啶并[2,3-D]嘧啶-6-甲酰胺;化合物A 484954;A 484954,CAM激酶III(EEF-2激酶)抑制剂 |
| 英文名称 | 7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide |
| 英文同义词 | 7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide;7-AMino-1-cyclopropyl-3-ethyl-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide;A-484954(A 484954);A 484954;7-Amino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxo-pyrido[2,3-d]pyrimidine-6-carboxamideddd;eEF2K Inhibitor, A-484954;7-Amino-1-cyclopropyl-3-ethyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-6-carboxamid;Pyrido[2,3-d]pyrimidine-6-carboxamide, 7-amino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxo- |
| CAS号 | 142557-61-7 |
| 分子式 | C13H15N5O3 |
| 分子量 | 289.29 |
| EINECS号 | |
| 相关类别 | 抑制剂;Agro-Products;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals |
| Mol文件 | 142557-61-7.mol |
| 结构式 |  |
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 |
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 |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-110096 | A-484954 | 1 mg | 380元 | |
| 2024/04/30 | HY-110096 | A-484954 A-484954 | 142557-61-7 | 5mg | 1000元 |