186971-69-7
| 中文名称 | 186971-69-7 |
|---|---|
| 中文同义词 | 化合物 T13065;化合物 TAK-024 |
| 英文名称 | TAK 024 |
| 英文同义词 | TAK 024;1-Piperazineacetic acid, 4-[2-[[4-[(aminoiminomethyl)amino]benzoyl]amino]acetyl]-3-[3-[[4-[(aminoiminomethyl)amino]benzoyl]amino]propyl]-2-oxo-, (3S)-;TAK 024,TAK024 |
| CAS号 | 186971-69-7 |
| 分子式 | C27H34N10O6 |
| 分子量 | 594.62 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 186971-69-7.mol |
| 结构式 |  |
186971-69-7 性质
| 熔点 | 245-251.5 °C |
|---|---|
| 密度 | 1.51±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 3.66±0.10(Predicted) |
IC50: 31 nM (human platelet), 79 nM (monkey platelet), 51 nM (pig platelet)
TAK-024 is a platelet inhibitor with IC 50 s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively. In a preliminary experiment, the IC 50 value of TAK-024 in the heparinized blood sample is 230 nM, 4.5-fold less potent than that in the citrated physiological blood sample. The ID 50 value of TAK-024 on ex vivo ADP-induced platelet aggregation in guinea pigs is 0.18 μg/kg/min, the dissociation ratio of TAK-024 is found to be 32.
Intravenous infusion of TAK-024 (compound 12c) at 1.6 μg/mL/min completely prevents arterial thrombus formation induced by endothelial injury in guinea pigs. Results demonstrate the inhibitory effects of TAK-024 on the carotid thrombosis induced by balloon injury in guinea pigs and the ID 50 value is 0.73 μg/kg/min. A single dose of TAK-024 at 100 μg/kg iv produces almost complete inhibition for 120 min, and about 40% inhibition is observed after 240 min. Dose-dependent inhibition of platelet aggregation is achieved with a single iv dose of 30 to 100 μg/kg of TAK-024.