Choose Your Country or Region

Riociguat

Synonyms: BAY 63-2521

Catalog No.S8135 Purity: 99.94%

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

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

Riociguat Related Products

Related Compound Libraries	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Bioactive Compound Library-Ⅱ GPCR Compound Library	Click to Expand

Choose Selective Guanylate Cyclase Inhibitors

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References
[1] Schermuly RT, et al. Eur Respir J. 2008, 32(4), 881-891. [2] Reiss C, et al. Br J Pharmacol. 2015, 172(21), 5199-5210. [3] Reinke Y, et al. Eur J Pharmacol. 2015, 767, 1-9.

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):