生物活性 | |||
---|---|---|---|
描述 | Riociguat is a potent sGC (soluble guanylate cyclase) stimulator with improved DMPK profile, used for the treatment of pulmonary hypertension[7]. It directly stimulates sGC and sensitises it to its physiological stimulator, nitric oxide[8]. It achieved threefold stimulation of cGMP formation in a recombinant sGC-overexpressing cell line with minimal effective concentration of 30nM[7]. Oral administration of BAY 63-2521 at 10 mg/kg/day partially reversed the pulmonary arterial hypertension induced by monocrotaline in rats or in chronic treatment of hypoxic mice. The reversion of the right heart hypertrophy and the structural remodelling of the lung vasculature could also be observed[8]. |
实验方案 | |||
---|---|---|---|
1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.37mL 0.47mL 0.24mL |
11.84mL 2.37mL 1.18mL |
23.67mL 4.73mL 2.37mL |
参考文献 |
---|