Riociguat (BAY 63-2521)

Catalog No.S8135

For research use only.

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

Riociguat (BAY 63-2521) Chemical Structure

CAS No. 625115-55-1

Selleck's Riociguat (BAY 63-2521) has been cited by 7 Publications

Purity & Quality Control

Choose Selective Guanylate Cyclase Inhibitors

Biological Activity

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

Protocol (from reference)

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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 422.42
Formula

C20H19FN8O2

CAS No. 625115-55-1
Storage 3 years -20°C powder
2 years -80°C in solvent
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
NCT04813926 Recruiting Drug: Riociguat (Adempas BAY63-2521) Pulmonary Arterial Hypertension Bayer|Xcenda LLC July 16 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
NCT02562235 Active not recruiting Drug: Riociguat (Adempas BAY63-2521) Hypertension Pulmonary Bayer|Merck Sharp & Dohme LLC October 29 2015 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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