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BIX 02565

CAS No. : 1311367-27-7

MCE 站：BIX 02565

产品活性：BIX 02565 是一种有效的核糖体 S6 激酶 2 (RSK2) 抑制剂，IC₅₀ 为 1.1 nM。

研究领域：MAPK/ERK Pathway

作用靶点：Ribosomal S6 Kinase (RSK)

In Vitro: 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.

In Vivo: 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 T_max). 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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