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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]. |
Dose | Rat; 0.1 mg/kg[3] (i.v.); 10 mg/kg[4] (p.o.) Mice: 30 mg/kg[5] (p.o.) | ||||||||
Administration | i.v., p.o. | ||||||||
Pharmacokinetics |
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计算器 | ||||
存储液制备 | 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 |
CAS号 | 625115-55-1 |
分子式 | C20H19FN8O2 |
分子量 | 422.416 |
别名 | BAY 632521 |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 18 mg/mL(42.61 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |