SB-772077B (hydrochloride)

ROCK抑制剂（ROCK1和ROCK2的IC50s分别为5.6和6nM）；对ROCK1和ROCK2具有选择性，而对Akt1、Akt2和Akt3的IC50s分别为324、1,950和1,290nM），以及对Cdk2、GSK3α、IKKβ、JNK3和Plk的IC50s均为≥7,000nM，但也抑制RSK1和MSK1（IC50s分别为35和14nM）；抑制LPS诱导的THP-1细胞中TNF-α和IL-6的产生；诱导预收缩的大鼠分离主动脉环松弛（IC50=39nM）；以剂量依赖性方式降低自发性高血压大鼠的血压，并以1mg/kg的剂量降低DOCA盐高血压大鼠的血压；以30、100和300μg/kg的剂量静脉注射，降低正常血压大鼠和野百合碱诱发的肺动脉高压大鼠的肺动脉和体循环动脉压，增加心输出量。A ROCK inhibitor (IC50s = 5.6 and 6 nM for ROCK1 and ROCK2, respectively); selective for ROCK1 and ROCK2 over Akt1, Akt2, and Akt3 (IC50s = 324, 1,950, and 1,290 nM, respectively), as well as Cdk2, GSK3α, IKKβ, JNK3, and Plk (IC50s = ≥7,000 nM for all), but also inhibits RSK1 and MSK1 (IC50s = 35 and 14 nM, respectively); inhibits LPS-induced TNF-α and IL-6 production in THP-1 cells; induces relaxation of pre-contracted isolated rat aortic rings (IC50 = 39 nM); reduces blood pressure in spontaneously hypertensive rats in a dose-dependent manner and in DOCA-salt hypertensive rats at 1 mg/kg; reduces pulmonary and systemic arterial pressure and increases cardiac output in normotensive rats and rats with monocrotaline-induced pulmonary hypertension at 30, 100, and 300 μg/kg, i.v.分子式C15H18N8O2 • 2HCl分子量415.3O=C(N1CC[C@H](N)C1)C2=C3C(N=C(C4=NON=C4N)N3CC)=CN=C2.Cl.Cl