Riociguat (BAY 63-2521)

For research use only.

Catalog No.S8135

5 publications

Riociguat (BAY 63-2521) Chemical Structure

CAS No. 625115-55-1

Riociguat (BAY 63-2521) is an oral soluble guanylate cyclase (GC) stimulator, used in the treatment of ipulmonary hypertension.

Selleck's Riociguat (BAY 63-2521) has been cited by 5 publications

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Biological Activity

Description Riociguat (BAY 63-2521) is an oral soluble guanylate cyclase (GC) stimulator, used in the treatment of ipulmonary hypertension.
guanylate cyclase [1]
In vitro

BAY 63-2521 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] [3]

In vivo In chronic treatment of hypoxic mice and MCT-injected rats, 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. [1]


Animal Research:[1]
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  • Animal Models: Chronic hypoxic mice, and monocrotaline (MCT)-injected rats
  • Dosages: 10 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 84 mg/mL (198.85 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 422.42


CAS No. 625115-55-1
Storage powder
in solvent
Synonyms N/A
Smiles CN(C1=C(N=C(N=C1N)C2=NN(C3=C2C=CC=N3)CC4=CC=CC=C4F)N)C(=O)OC

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04954742 Not yet recruiting Drug: Riociguat Primary Pulmonary Arterial Hypertension|Chronic Thromboembolic Pulmonary Hypertension Heidelberg University|Merck Sharp & Dohme Corp. September 2021 Phase 4
NCT04813926 Not yet recruiting Drug: Riociguat (Adempas BAY63-2521) Pulmonary Arterial Hypertension Bayer|Xcenda LLC August 23 2021 --
NCT04780932 Recruiting Drug: Macitentan 10mg|Drug: Placebo Thromboembolic Pulmonary Hypertension|Chronic Disease|Inoperable Disease Assistance Publique - Hôpitaux de Paris|Janssen LP June 14 2021 Phase 2|Phase 3
NCT03389321 Completed Drug: Riociguat (Adempas)|Drug: Macitentan (Opsumit) Healthy Subjects Actelion January 9 2018 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID