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186971-69-7

中文名稱(chēng) 186971-69-7
英文名稱(chēng) TAK 024
CAS 186971-69-7
分子式 C27H34N10O6
分子量 594.62
MOL 文件 186971-69-7.mol
186971-69-7 結(jié)構(gòu)式 186971-69-7 結(jié)構(gòu)式

基本信息

中文別名
化合物 T13065
英文別名
TAK 024
1-Piperazineacetic acid, 4-[2-[[4-[(aminoiminomethyl)amino]benzoyl]amino]acetyl]-3-[3-[[4-[(aminoiminomethyl)amino]benzoyl]amino]propyl]-2-oxo-, (3S)-

物理化學(xué)性質(zhì)

熔點(diǎn)245-251.5 °C
密度1.51±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)3.66±0.10(Predicted)

常見(jiàn)問(wèn)題列表

生物活性
TAK-024 是一種血小板抑制劑,在人,猴和豚鼠中的 IC50 值分別為 31, 79 和 51 nM。
靶點(diǎn)

IC50: 31 nM (human platelet), 79 nM (monkey platelet), 51 nM (pig platelet)

體外研究

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.

體內(nèi)研究

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.

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