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TAK-024
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TAK-024图片
CAS NO:186971-69-7
规格:98%
分子量:594.62
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
TAK-024是一种血小板抑制剂,在人,猴和豚鼠中的IC50值分别为31,79和51nM。
CAS:186971-69-7
分子式:C27H34N10O6
分子量:594.62
纯度:98%
存储:Store at -20°C

Background:

TAK-024 is a platelet inhibitor with IC50s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively.


TAK-024 is a platelet inhibitor with IC50s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively. In a preliminary experiment, the IC50 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 ID50 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[1].


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 ID50 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[1].


[1]. Kitamura S, et al. Potent dibasic GPIIb/IIIa antagonists with reduced prolongation of bleeding time: synthesis and pharmacological evaluation of 2-oxopiperazine derivatives. J Med Chem. 2001 Jul 19;44(15):2438-50.