Art. -Nr.: HY-14779

Riociguat

Name: Riociguat
Brand: MedChemExpress
SKU: HY-14779
Price: 79.00 USD
Availability: InStock
Rating: 5 (20 reviews)

(Synonyms: BAY 632521)

20 Cited Publications

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Based on 20 publication(s) in Google Scholar

Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.80%
CAS. Nr.: 625115-55-1
Formel: C₂₀H₁₉FN₈O₂
Molecular Weight:422.42

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Riociguat Chemical Structure

CAS. Nr.: 625115-55-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (20)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension.

IC₅₀ & Target

sGC^[1]

In Vitro

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.

In Vivo

Riociguat (10 mg/kg/d, p.o.) partially reverses the pulmonary arterial hypertension, the right heart hypertrophy and the structural remodelling of the lung vasculature in chronic treatment of hypoxic mice and MCT-injected rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 625115-55-1
Appearance Solid
Molecular Weight 422.42
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (20)

All Bio/Physico-chemical AssayELISART-PCRWB

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Journal Impact Factor

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
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
Br J Pharmacol

Oxidized soluble guanylyl cyclase causes erectile dysfunction in alcoholic mice. [Abstract]

2023 Sep;180(18):2361-2376. PMID: 37021655

Riociguat purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2023 Sep;180(18):2361-2376. [Abstract]

Effects of exposure to vehicle (0.001% DMSO) or Riociguat (30 nM; 5 min) on cGMP content in penis tissues from control and alcoholic mice (n = 8, two-way ANOVA results are shown in the table).
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

Riociguat purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2019 Jul;176(13):2131-2145. [Abstract]

Representative traces and mean values of Kv currents recorded after the application of depolarizing ramps from −60 to +20 mV in the absence or the presence of Riociguat (0.3 μM, n = 15 from eight animals). Inset shows the current density at −30 mV before and after the addition of Riociguat. Riociguat induced a substantial increase in K⁺ currents at all potentials ≥−40 mV within the first 1–2 min and reached a stable effect at 5–7 min.
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

Riociguat purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 Mar 5:248:117866. [Abstract]

cGMP production in HBECs treated with different concentrations of Riociguat (Rio, 100 nM-10 μM) with or without sildenafil for 1 or 24 h. In HBECs treated with Riociguat, co-incubation with sildenafil increased cGMP production at all concentrations after 1 and 24 h.

Riociguat purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 Mar 5:248:117866. [Abstract]

HBECs were incubated for 15 min with sildenafil 1 µM, followed by 15 min with cinaciguat or Riociguat (100 nM, 1 µM, and 10 µM), in the presence or absence of sildenafil, and then stimulated with CSE for 24 h. NOX4 gene expression was quantified by reverse transcription (RT) and real-time PCR. Data are expressed as 2^{^−ΔΔCt}.
Int J Mol Sci

Mitochondrial Abundant Heat Soluble (MAHS) Protein Expression Modulates Metabolic Dynamics in Human Adipose-Derived Stem Cells. [Abstract]

2026 Jul 15;27(14):6289. PMID: 42511631
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.
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
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
Am J Physiol Lung Cell Mol Physiol

Newborn rat response to single vs. combined cGMP-dependent pulmonary vasodilators. [Abstract]

2014 Jan;306(2):L207-15. PMID: 24242011
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
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
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
Biomed Pharmacother

Revisiting soluble guanylate cyclase pharmacology: Additive potential of stimulators and activators. [Abstract]

2025 Dec:193:118762. PMID: 41252787
Patent

US20250281485A1.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3673 mL

11.8366 mL

23.6731 mL

5 mM

0.4735 mL

2.3673 mL

4.7346 mL

10 mM

0.2367 mL

1.1837 mL

2.3673 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2 mg/mL (4.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Protokoll

Animal Administration^[1]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

Riociguat

20 Cited Publications

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Riociguat

Publications Citing Use of MedChemExpress (MCE) Riociguat