1. GPCR/G Protein
  2. Guanylate Cyclase
  3. Riociguat

Riociguat (Synonyms: BAY 632521)

Cat. No.: HY-14779 Purity: 99.58%
Handling Instructions

Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) 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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10 mM * 1 mL in DMSO USD 79 In-stock
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10 mg USD 108 In-stock
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50 mg USD 288 In-stock
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100 mg USD 480 In-stock
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200 mg USD 768 In-stock
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Customer Review

Based on 11 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Riociguat purchased from MCE. Usage Cited in: PLoS One. 2018 Jul 10;13(7):e0199927.

    Riociguat (Rio) decreases hyperoxia-induced vascular remodeling. Representative Western blots of CTGF and β-actin.

    Riociguat purchased from MCE. Usage Cited in: Sci Rep. 2018 Jun 19;8(1):9372.

    Effects of Riociguat (RIO) on protein expression in early CCl4 rats.
    • Biological Activity

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    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    sGC[1]

    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
    Molecular Weight

    422.42

    Formula

    C₂₀H₁₉FN₈O₂

    CAS No.

    625115-55-1

    SMILES

    FC1=CC=CC=C1CN2C3=NC=CC=C3C(C4=NC(N)=C(C(N)=N4)N(C)C(OC)=O)=N2

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (118.37 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent 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.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.92 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.92 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.92 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Animal Administration
    [1]

    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).
    Rats[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

    Purity: 99.58%

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    Product name:
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    Cat. No.:
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