Riociguat
Based on 19 publication(s) in Google Scholar
Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension.
For research use only. We do not sell to patients.
- Purity: 99.80%
- CAS No.: 625115-55-1
- Formula: C20H19FN8O2
- Molecular Weight:422.42
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocol
- Purity & Documentation
- References
-
Help & FAQs
-
GPCR/G Protein Compound Library
HY-L006
-
FDA-Approved Drug Library
HY-L022
-
Drug Repurposing Compound Library
HY-L035
-
Anti-Cardiovascular Disease Compound Library
HY-L046
-
Anti-COVID-19 Compound Library
HY-L052
-
NMPA-Approved Drug Library
HY-L053
-
Orally Active Compound Library
HY-L061
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Rare Diseases Drug Library
HY-L102
-
EMA-Approved Drug Library
HY-L116
-
Human Metabolite Library
HY-L123
-
Heterocyclic Compound Library
HY-L138
-
Withdrawn Drug Compound Library
HY-L140
-
Off-patent Drug Library
HY-L141
-
Antihypertensive Compound Library
HY-L145
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
FDA-Approved Drug Library Plus
HY-L022P
-
FDA-Approved Drug Library Mini
HY-L022M
-
Bioactive Compound Library
HY-L001
-
Protein Kinase Compound Library
HY-L196
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
RNA Binding Bioactive Compound Library
HY-L248
-
Lactylation Compound Library
HY-L249
-
Classic FDA-Approved Drug Library
HY-L261
Publications Citing Use of MedChemExpress (MCE) Riociguat
More- Nat Commun. 2018 Oct 16;9(1):4301. [Abstract]
- Br J Pharmacol. 2023 Sep;180(18):2361-2376. [Abstract]
- Br J Pharmacol. 2019 Jul;176(13):2131-2145. [Abstract]
- Biomed Pharmacother. 2025 Nov 17:193:118762. [Abstract]
- Diabetes. 2018 Apr;67(4):607-623. [Abstract]
- Antioxidants (Basel). 2021 Jan 21;10(2):155. [Abstract]
- Biochem Pharmacol. 2026 Mar 5:248:117866. [Abstract]
- J Physiol. 2019 Feb;597(4):1087-1101. [Abstract]
- Sci Rep. 2018 Jun 19;8(1):9372. [Abstract]
- Am J Physiol Lung Cell Mol Physiol. 2014 Jan;306(2):L207-15. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2025 Feb 1:1252:124443. [Abstract]
- Pulm Pharmacol Ther. 2014 Aug;28(2):130-7. [Abstract]
- PLoS One. 2018 Jul 10;13(7):e0199927. [Abstract]
- PLoS One. 2018 Jan 24;13(1):e0191239. [Abstract]
- Vet Sci. 2023 Feb 15;10(2):159. [Abstract]
- Physiol Rep. 2023 Jan;11(1):e15549. [Abstract]
- Physiol Rep. 2022 Jan;10(1):e15156. [Abstract]
- Exp Lung Res. 2021 Oct;47(8):382-389. [Abstract]
- Patent. US20250281485A1.
Customer Validation & Images
-
WB
-
WB
Biological Activity
sGC[1]
Riocigua stimulates the recombinant sGC concentration dependently from 0.1 to 100 μM with a two-fold to 73-fold effect by an NO-independent but haem-dependent mechanism[1]. Riociguat inhibits platelet function in washed platelets but not in whole blood, and exerts no direct effects on contractility and relaxation of cardiac myocytes[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 625115-55-1
-
Appearance Solid
-
Molecular Weight 422.42
-
Formula C20H19FN8O2
-
Color Off-white to yellow
-
SMILES
FC1=CC=CC=C1CN2C3=NC=CC=C3C(C4=NC(N)=C(C(N)=N4)N(C)C(OC)=O)=N2
-
Synonyms
BAY 632521
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (19)
-
Journal Impact Factor
-
Most Recent
-
Nat Commun
A shear-dependent NO-cGMP-cGKI cascade in platelets acts as an auto-regulatory brake of thrombosis. [Abstract]2018 Oct 16;9(1):4301. PMID: 30327468 -
Br J Pharmacol
2023 Sep;180(18):2361-2376. PMID: 37021655 -
Br J Pharmacol
Activation of Kv 7 channels as a novel mechanism for NO/cGMP-induced pulmonary vasodilation. [Abstract]2019 Jul;176(13):2131-2145. PMID: 30883701 -
Biomed Pharmacother
Revisiting soluble guanylate cyclase pharmacology: Additive potential of stimulators and activators. [Abstract]2025 Nov 17:193:118762. PMID: 41252787 -
Diabetes
Protein Kinase G Activation Reverses Oxidative Stress and Restores Osteoblast Function and Bone Formation in Male Mice With Type 1 Diabetes. [Abstract]2018 Apr;67(4):607-623. PMID: 29301852 -
Antioxidants (Basel)
Oxygen-sensitivity and Pulmonary Selectivity of Vasodilators as Potential Drugs for Pulmonary Hypertension. [Abstract]2021 Jan 21;10(2):155. PMID: 33494520 -
Biochem Pharmacol
Differential modulation of the sGC-cGMP pathway by sGC stimulators and activators in human lung cells. [Abstract]2026 Mar 5:248:117866. PMID: 41794266 -
J Physiol
Characterization and regulation of wild-type and mutant TASK-1 two pore domain potassium channels indicated in pulmonary arterial hypertension. [Abstract]2019 Feb;597(4):1087-1101. PMID: 30365877 -
Sci Rep
The soluble guanylate cyclase stimulator riociguat reduces fibrogenesis and portal pressure in cirrhotic rats. [Abstract]2018 Jun 19;8(1):9372. PMID: 29921982
Riociguat purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Jun 19;8(1):9372. [Abstract]
Effects of Riociguat (RIO) on protein expression in early CCl4 rats.
-
Am J Physiol Lung Cell Mol Physiol
2014 Jan;306(2):L207-15. PMID: 24242011 -
J Chromatogr B Analyt Technol Biomed Life Sci
A simple HPLC-UV method for monitoring therapeutic adherence in pulmonary arterial hypertension. [Abstract]2025 Feb 1:1252:124443. PMID: 39787725 -
Pulm Pharmacol Ther
Pharmacokinetic interaction profile of riociguat, a new soluble guanylate cyclase stimulator, in vitro. [Abstract]2014 Aug;28(2):130-7. PMID: 24657506 -
PLoS One
Riociguat prevents hyperoxia-induced lung injury and pulmonary hypertension in neonatal rats without effects on long bone growth. [Abstract]2018 Jul 10;13(7):e0199927. PMID: 29990355
Riociguat purchased from MedChemExpress. Usage Cited in: PLoS One. 2018 Jul 10;13(7):e0199927. [Abstract]
Riociguat (Rio) decreases hyperoxia-induced vascular remodeling. Representative Western blots of CTGF and β-actin.
-
PLoS One
Riociguat versus sildenafil on hypoxic pulmonary vasoconstriction and ventilation/perfusion matching. [Abstract]2018 Jan 24;13(1):e0191239. PMID: 29364918 -
Vet Sci
Effects of a Soluble Guanylate Cyclase Stimulator Riociguat on Contractility of Isolated Pulmonary Artery and Hemodynamics of U46619-Induced Pulmonary Hypertension in Dogs. [Abstract]2023 Feb 15;10(2):159. PMID: 36851463 -
Physiol Rep
β3 adrenergic agonism: A novel pathway which improves right ventricular-pulmonary arterial hemodynamics in pulmonary arterial hypertension. [Abstract]2023 Jan;11(1):e15549. PMID: 36597221 -
Physiol Rep
Modulation of soluble guanylate cyclase ameliorates pulmonary hypertension in a rat model of chronic thromboembolic pulmonary hypertension by stimulating angiogenesis. [Abstract]2022 Jan;10(1):e15156. PMID: 35001565 -
Exp Lung Res
Riociguat can ameliorate bronchopulmonary dysplasia in the SU5416 induced rat experimental model. [Abstract]2021 Oct;47(8):382-389. PMID: 34528477 -
Solvent & Solubility
DMSO : 20 mg/mL (47.35 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (4.73 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2 mg/mL (4.73 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Mice[1]
For chronic intervention studies four groups of mice are used: control mice exposed for 35 days to normoxic gas (n=10); mice exposed for 21 days to hypoxic gas (n=10); mice exposed for 35 days to hypoxic gas and who receives the vehicle (2% methylcellulose solution) from day 21 to day 35 (n=10); and mice exposed for 35 days to hypoxic gas and who receives BAY 63-2521 (10 mg/kg) once a day by oral application (n=10) from day 21 to day 35. For continuous measurement of Prvs and cardiac frequency by radiotelemetry, a separate group of mice is exposed for 35 days to hypoxic gas and receives BAY 63-2521 (10 mg/kg) once a day by oral application from day 21 to day 35. In order to investigate vascular reactivity in isolated mouse lungs, an additional two groups of animals are investigated: control mice (n=12) and animals exposed for 21 days to hypoxic conditions (n=12).
Rats[1]
Rats are randomised for chronic BAY 63-2521 treatment, 21 days after MCT injection. The experimental groups includes rats that receives BAY 63-2521 (10 mg/kg) or vehicle (2% methylcellulose solution) by oral application, once per day. Rats are examined daily and subjected to haemodynamic measurements and histological assessment at day 35.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
-
Data Sheet (283 KB)
-
SDS (788 KB)
- English - EN (788 KB)
- Français - FR (788 KB)
- Deutsch - DE (788 KB)
- Norwegian - NO (788 KB)
- Español - ES (788 KB)
- Swedish - SV (788 KB)
- Italian - IT (788 KB)
- Korean - KR (788 KB)
- Portuguese - PT (788 KB)
-
Handling Instructions (2659 KB)
References
[1]. Schermuly RT, et al. Expression and function of soluble guanylate cyclase in pulmonary arterial hypertension. Eur Respir J. 2008 Oct;32(4):881-91. [Content Brief]
[2]. Schermuly RT, et al. Riociguat for the treatment of pulmonary hypertension. Expert Opin Investig Drugs. 2011 Apr;20(4):567-76. [Content Brief]
[3]. Donda K, et al. Riociguat prevents hyperoxia-induced lung injury and pulmonary hypertension in neonatal rats without effects on long bone growth. PLoS One. 2018 Jul 10;13(7):e0199927. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3673 mL | 11.8366 mL | 23.6731 mL | 59.1828 mL |
| 5 mM | 0.4735 mL | 2.3673 mL | 4.7346 mL | 11.8366 mL | |
| 10 mM | 0.2367 mL | 1.1837 mL | 2.3673 mL | 5.9183 mL | |
| 15 mM | 0.1578 mL | 0.7891 mL | 1.5782 mL | 3.9455 mL | |
| 20 mM | 0.1184 mL | 0.5918 mL | 1.1837 mL | 2.9591 mL | |
| 25 mM | 0.0947 mL | 0.4735 mL | 0.9469 mL | 2.3673 mL | |
| 30 mM | 0.0789 mL | 0.3946 mL | 0.7891 mL | 1.9728 mL | |
| 40 mM | 0.0592 mL | 0.2959 mL | 0.5918 mL | 1.4796 mL |
Riociguat Related Classifications
HY-14779 Related Classifications
Powered by Bioz