Home GPCR & G Protein Guanylate Cyclase agonist Riociguat For research use only.

Riociguat

Synonyms: BAY 63-2521

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

Riociguat Chemical Structure

Riociguat Chemical Structure

CAS: 625115-55-1

Selleck's Riociguat has been cited by 9 publications

Purity & Quality Control

Batch: Purity: 99.94%
99.94

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Biological Activity

Description Riociguat is an oral soluble guanylate cyclase (GC) stimulator, used in the treatment of ipulmonary hypertension.
Targets
guanylate cyclase [1]
In vitro
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 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 Animal Models Chronic hypoxic mice, and monocrotaline (MCT)-injected rats
Dosages 10 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05750446 Not yet recruiting Migraine Without Aura Danish Headache Center April 1 2023 Not Applicable
NCT05582811 Completed Headache Danish Headache Center October 26 2022 Not Applicable
NCT04813926 Recruiting Pulmonary Arterial Hypertension Bayer|Xcenda LLC July 16 2021 --
NCT04780932 Recruiting Thromboembolic Pulmonary Hypertension|Chronic Disease|Inoperable Disease Assistance Publique - Hôpitaux de Paris|Janssen LP June 14 2021 Phase 2|Phase 3
NCT03389321 Completed Healthy Subjects Actelion January 9 2018 Phase 1

Chemical lnformation & Solubility

Molecular Weight 422.42 Formula

C20H19FN8O2
CAS No. 625115-55-1 SDF Download Riociguat SDF
Smiles CN(C1=C(N=C(N=C1N)C2=NN(C3=C2C=CC=N3)CC4=CC=CC=C4F)N)C(=O)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 84 mg/mL ( (198.85 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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