Riociguat (BAY 63-2521)

Catalog No.S8135

Riociguat (BAY 63-2521) Chemical Structure

Molecular Weight(MW): 422.42

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

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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.
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

Animal Research:[1]
+ Expand
  • Animal Models: Chronic hypoxic mice, and monocrotaline (MCT)-injected rats
  • Formulation: 2% methylcellulose solution
  • 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
Formula

C20H19FN8O2

CAS No. 625115-55-1
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03273257 Recruiting Chronic Thromboembolic Pulmonary Hypertension|CTEPH International CTEPH Association August 17 2018 Phase 2
NCT03273257 Recruiting Chronic Thromboembolic Pulmonary Hypertension|CTEPH International CTEPH Association August 17 2018 Phase 2
NCT03389321 Completed Healthy Subjects Actelion January 9 2018 Phase 1
NCT03389321 Completed Healthy Subjects Actelion January 9 2018 Phase 1
NCT02633397 Recruiting Sickle Cell Disease Gregory J. Kato MD|University of Pittsburgh April 11 2017 Phase 2
NCT02633397 Recruiting Sickle Cell Disease Gregory J. Kato MD|University of Pittsburgh April 11 2017 Phase 2

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID