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
500 mg   Get quote  
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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
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References
Preparing Stock Solutions
Concentration Volume 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
Please refer to the solubility information to select the appropriate solvent.
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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