1. GPCR/G Protein
  2. Guanylate Cyclase

Riociguat (Synonyms: BAY 632521)

Cat. No.: HY-14779 Purity: 99.73%
Data Sheet SDS Handling Instructions

Riociguat is an oral stimulator of soluble guanylate cyclase (sGC), and used in the treatment of pulmonary hypertension.

For research use only. We do not sell to patients.
Riociguat Chemical Structure

Riociguat Chemical Structure

CAS No. : 625115-55-1

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $66 In-stock
5 mg $60 In-stock
10 mg $90 In-stock
50 mg $240 In-stock
100 mg $400 In-stock
200 mg $640 In-stock
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Description

Riociguat is an oral stimulator of soluble guanylate cyclase (sGC), and used in the treatment of pulmonary hypertension.

In Vitro

Riocigua 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].

In Vivo

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 in chronic treatment of hypoxic mice and MCT-injected rats[1].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02915835 Dinesh Khanna, MD, MS|Bayer|University of Michigan Scleroderma|Digital Ulcers September 2016 Phase 2
NCT02117791 Bayer Hypertension, Pulmonary July 16, 2014
NCT02024386 Richard Moon|Duke University Hypertension, Pulmonary|Altitude Sickness January 2014 Phase 4
NCT02633397 Gregory J. Kato, MD|University of Pittsburgh Sickle Cell Disease April 11, 2017 Phase 2
NCT02428985 Bayer Hypertension, Pulmonary June 29, 2015
NCT02744339 Medical University of Vienna Hypertension, Pulmonary|Heart Failure With Normal Ejection Fraction March 2016 Phase 2
NCT02007629 Bayer Hypertension, Pulmonary February 2014 Phase 3
NCT02634203 Assistance Publique - Hôpitaux de Paris|Bayer Chronic Thromboembolic Pulmonary Hypertension January 2016
NCT00855660 Bayer Pharmacology, Clinical March 2009 Phase 1
NCT02625558 University of Cincinnati Sarcoidosis April 2015 Phase 4
NCT02562235 Bayer|Merck Sharp & Dohme Corp. Hypertension, Pulmonary October 29, 2015 Phase 3
NCT01179334 Bayer Pulmonary Hypertension August 2010 Phase 2
NCT01165931 Bayer Coronary Artery Disease May 2012 Phase 2
NCT02283762 Bayer Scleroderma, Systemic January 15, 2015 Phase 2
NCT02138825 Bayer Idiopathic Interstitial Pneumonias / Hypertension,Pulmonary June 4, 2014 Phase 2
NCT02159326 Bayer Drug Interactions June 2014 Phase 1
NCT01065051 Bayer Hypertension, Pulmonary|Ventricular Dysfunction, Left November 2010 Phase 2
NCT02759419 Bayer Hypertension, Pulmonary June 16, 2016 Phase 4
NCT01784562 Bayer Hypertension, Pulmonary
NCT02092818 Bayer Hypertension, Pulmonary May 31, 2014
NCT02891850 Bayer Pulmonary Arterial Hypertension January 12, 2017 Phase 4
NCT01065454 Bayer Hypertension, Pulmonary|Ventricular Dysfunction, Left April 14, 2010 Phase 2
NCT00640315 Bayer Hypertension, Pulmonary|Pulmonary Disease, Chronic Obstructive August 2008 Phase 1
NCT00855465 Bayer Pulmonary Hypertension February 2009 Phase 3
NCT02159313 Bayer Healthy Volunteers June 2014 Phase 1
NCT02545465 Bayer Hypertension, Pulmonary September 15, 2015
NCT01172756 Bayer Hypertension, Pulmonary|Ventricular Dysfunction, Left July 2010 Phase 2
NCT00810693 Bayer Pulmonary Hypertension December 2008 Phase 3
NCT02170025 Bayer|Merck Sharp & Dohme Corp. Cystic Fibrosis September 30, 2014 Phase 2
NCT00910429 Bayer Pulmonary Hypertension July 1, 2009 Phase 3
NCT00863681 Bayer Hypertension, Pulmonary March 12, 2009 Phase 3
NCT00694850 Bayer Hypertension, Pulmonary August 2, 2008 Phase 2
NCT01926847 Bayer Raynaud Disease October 2013 Phase 2
NCT00454558 Bayer Hypertension, Pulmonary January 2007 Phase 2
NCT00680654 Bayer Hypertension, Pulmonary October 2008 Phase 1
NCT02191137 Bayer Hypertension, Pulmonary September 2014 Phase 4
NCT02556268 Bayer HIV-DDI February 2016 Phase 1
NCT01489488 Bayer Pharmacology, Clinical January 2012 Phase 1
NCT03074539 Medical University of Vienna Chronic Thromboembolic Pulmonary Hypertension|Sleep Disordered Breathing February 1, 2017
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.3673 mL 11.8366 mL 23.6731 mL
5 mM 0.4735 mL 2.3673 mL 4.7346 mL
10 mM 0.2367 mL 1.1837 mL 2.3673 mL
Animal Administration
[1]

Riociguat is formulated in 2% methylcellulose.

Mice[1]
For chronic intervention studies four groups of mice are used: control mice exposed for 35 days to normoxic gas (n=10); mice exposed for 21 days to hypoxic gas (n=10); mice exposed for 35 days to hypoxic gas and who receives the vehicle (2% methylcellulose solution) from day 21 to day 35 (n=10); and mice exposed for 35 days to hypoxic gas and who receives BAY 63-2521 (10 mg/kg) once a day by oral application (n=10) from day 21 to day 35. For continuous measurement of Prvs and cardiac frequency by radiotelemetry, a separate group of mice is exposed for 35 days to hypoxic gas and receives BAY 63-2521 (10 mg/kg) once a day by oral application from day 21 to day 35. In order to investigate vascular reactivity in isolated mouse lungs, an additional two groups of animals are investigated: control mice (n=12) and animals exposed for 21 days to hypoxic conditions (n=12).
Rat[1]
Rats are randomised for chronic BAY 63-2521 treatment, 21 days after MCT injection. The experimental groups includes rats that receives BAY 63-2521 (10 mg/kg) or vehicle (2% methylcellulose solution) by oral application, once per day. Rats are examined daily and subjected to haemodynamic measurements and histological assessment at day 35. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

422.42

Formula

C₂₀H₁₉FN₈O₂

CAS No.

625115-55-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.73%

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Product Name:
Riociguat
Cat. No.:
HY-14779
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