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

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Riociguat/利奥西呱 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/利奥西呱 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/利奥西呱 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/利奥西呱 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/利奥西呱 技术信息

CAS号625115-55-1
分子式C20H19FN8O2
分子量 422.42
SMILES Code O=C(OC)N(C1=C(N)N=C(C2=NN(CC3=CC=CC=C3F)C4=NC=CC=C42)N=C1N)C
MDL No. MFCD19443708
别名 BAY 632521
运输蓝冰
InChI Key WXXSNCNJFUAIDG-UHFFFAOYSA-N
Pubchem ID 11304743
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
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