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利奥西呱 /Riociguat {[allProObj[0].p_purity_real_show]}

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 CAS号:625115-55-1
Riociguat 化学结构
CAS号:625115-55-1
Riociguat 3D分子结构
CAS号:625115-55-1
Riociguat 化学结构 CAS号:625115-55-1
Riociguat 3D分子结构 CAS号:625115-55-1
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Riociguat 纯度/质量文件 产品仅供科研

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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]. 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].

Riociguat 动物研究

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
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.

Riociguat 实验方案

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

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

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

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
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