利奥西呱 /Riociguat
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货号：A255332
同义名：
BAY 632521
Riociguat是一种口服可用的可溶性鸟苷酸环化酶 (sGC) 刺激剂，用于治疗肺动脉高压。
Riociguat 化学结构
Riociguat 3D分子结构
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Riociguat 质控信息
Riociguat 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] [8] [7] [8]
Riociguat 动物研究
Dose
Rat； 0.1 mg/kg[3] [4] [5]
Administration
i.v., p.o.
Pharmacokinetics
Animal
Rats[6]
F
35% - 65%
CL
1.3 L/kg·h
Vdss
1.2 L/kg
Riociguat 参考文献
[1] Mittendorf J, Weigand S, et al. Discovery of riociguat (BAY 63-2521): a potent, oral stimulator of soluble guanylate cyclase for the treatment of pulmonary hypertension. ChemMedChem. 2009 May;4(5):853-65.
[2] Schermuly RT, Stasch JP, et al. Expression and function of soluble guanylate cyclase in pulmonary arterial hypertension. Eur Respir J. 2008 Oct;32(4):881-91.
[3] Chamorro V, Morales-Cano D, et al. Riociguat versus sildenafil on hypoxic pulmonary vasoconstriction and ventilation/perfusion matching. PLoS One. 2018 Jan 24;13(1):e0191239.
[4] Lang M, Kojonazarov B, et al. The soluble guanylate cyclase stimulator riociguat ameliorates pulmonary hypertension induced by hypoxia and SU5416 in rats. PLoS One. 2012;7(8):e43433.
[5] Rai N, Veeroju S, et al. Effect of Riociguat and Sildenafil on Right Heart Remodeling and Function in Pressure Overload Induced Model of Pulmonary Arterial Banding. Biomed Res Int. 2018 Jan 3;2018:3293584.
[6] BAY 63-2521
[7] Mittendorf J, Weigand S, Alonso-Alija C, Bischoff E, Feurer A, Gerisch M, Kern A, Knorr A, Lang D, Muenter K, Radtke M, Schirok H, Schlemmer KH, Stahl E, Straub A, Wunder F, Stasch JP. Discovery of riociguat (BAY 63-2521): a potent, oral stimulator of soluble guanylate cyclase for the treatment of pulmonary hypertension. ChemMedChem. 2009 May;4(5):853-65. doi: 10.1002/cmdc.200900014. PMID: 19263460.
[8] Schermuly RT, Stasch JP, Pullamsetti SS, Middendorff R, Müller D, Schlüter KD, Dingendorf A, Hackemack S, Kolosionek E, Kaulen C, Dumitrascu R, Weissmann N, Mittendorf J, Klepetko W, Seeger W, Ghofrani HA, Grimminger F. Expression and function of soluble guanylate cyclase in pulmonary arterial hypertension. Eur Respir J. 2008 Oct;32(4):881-91. doi: 10.1183/09031936.00114407. Epub 2008 Jun 11. PMID: 18550612.
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Riociguat 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
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
Riociguat 技术信息
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