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 No. 625115-55-1

Purity & Quality Control

Riociguat Related Products

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 Active not 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 Information & 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
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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.

Handling Instructions

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