BIX 02565CAS号: 1311367-27-7分子式: C26H30N6O2分子量: 458.5554描述纯度储存/保存方法别名外观靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
BIX 02565 is a novel ribosomal S6 kinase 2 (RSK2) inhibitor with an IC50 of 1.1 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 |
BIX-02565;BIX02565
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外观 |
Powder
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生物活性 | |
靶点 |
Ribosomal S6 Kinase (RSK)
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In vitro(体外研究) |
BIX 02565, a potent RSK2 inhibitor (IC50=1.1 nM) targets for the treatment of heart failure secondary to myocardial infarction through indirect NHE inhibition. BIX 02565, a second Rsk inhibitor, protects enzyme active sites from reaction with biotinylated nucleotide acyl phosphates.
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In vivo(体内研究) |
In telemetry-instrumented rats, BIX 02565 (30, 100, and 300 mg/kg p.o. QD for 4 days) elicits concentration-dependent decreases in MAP after each dose (to -39±4 mm Hg on day 4 at Tmax). BIX 02565 produces concentration-dependent relaxation ex vivo in the phenylephrine-constricted rat aortic ring at concentrations above 0.03 μM with a calculated EC50 of 3.1 μM. Subsequently, BIX 02565 is infused in the anesthetized rat in a low-dose (0.1, 0.3, and 1.0 mg/kg per 20 min) and high-dose (1.0, 3.0, and 10.0 mg/kg per 20 min) series of continuous infusions to test the effect of compound on hemodynamics in vivo.
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分子结构图