BIX 02565

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BIX 02565 是核糖体 S6 激酶 2 的有效抑制剂（RSK2，IC50：1.1 nM）。

BIX 02565 is a potent inhibitor of ribosomal S6 kinase 2 (RSK2 IC50: 1.1 nM).

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 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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PI3K/Akt/mTOR signaling

S6 Kinase

RSK2|LRRK2

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1311367-27-7

458.56

C26H30N6O2

>98% (HPLC)

DMSO: 20 mg/mL

C[C@@H]1CCNC(=O)c2cc3ccc(cc3n12)C(=O)Nc1nc2ccccc2n1CCCN(C)C

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(-20℃)

With Ice Pack

≥ 2 years