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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Riociguat (formerly also known as BAY-63-2521, BAY-632521; trade name Adempas) is a first-in-class and oral bioavailable soluble guanylate cyclase (GC) stimulator that has been approved to treat two forms of pulmonary hypertension (PH): chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH). Riociguat is the first medication in a brand-new class of sGC stimulators.
Targets |
sGC
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ln Vitro |
Riocigua works through a haem-dependent but NO-independent mechanism to stimulate the recombinant sGC concentration dependently from 0.1 to 100 μM with an effect ranging from two to 73 times[1]. Riociguat has no direct effects on the contractility and relaxation of cardiac myocytes, but it inhibits platelet function in washed platelets but not in whole blood[2].
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ln Vivo |
Riociguat (10 mg/kg/d, p.o.) partially reverses the pulmonary arterial hypertension, the hypertrophy of the right heart, and the structural remodeling of the lung vasculature in chronic treatment of hypoxic mice and MCT-injected rats[1].
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Animal Protocol |
Mice: Four groups of mice are used for the chronic intervention studies: ten control mice exposed to normoxic gas for 35 days; ten hypoxic gas exposed for 21 days; ten mice exposed for 35 days and given the vehicle (2% methylcellulose solution) from day 21 to day 35; and ten mice exposed for 35 days and given BAY 63-2521 (10 mg/kg) once daily by oral application from day 21 to day 35. In order to perform continuous radiotelemetry measurements of cardiac frequency and Prvs, a different group of mice is given oral application of BAY 63-2521 (10 mg/kg) once daily from day 21 to day 35 after being exposed to hypoxic gas for 35 days. Further two groups of animals are studied: control mice (n = 12) and animals exposed to hypoxia for 21 days (n = 12) in order to examine vascular reactivity in isolated mouse lungs.
Rats: One week following MCT injection, rats are randomly assigned to receive chronic BAY 63-2521 treatment. A vehicle (2% methylcellulose solution) or BAY 63-2521 (10 mg/kg) are administered orally to rats in the experimental groups once daily. On day 35, rats undergo histological evaluation and are monitored every day for the duration of their lives.
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References |
Molecular Formula |
C20H19FN8O2
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Molecular Weight |
422.42
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Exact Mass |
422.16
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Elemental Analysis |
C, 56.87; H, 4.53; F, 4.50; N, 26.53; O, 7.58
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CAS # |
625115-55-1
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Related CAS # |
Riociguat-13C,d6
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Appearance |
Light yellow solid powder
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SMILES |
CN(C1=C(N=C(N=C1N)C2=NN(C3=C2C=CC=N3)CC4=CC=CC=C4F)N)C(=O)OC
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InChi Key |
WXXSNCNJFUAIDG-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C20H19FN8O2/c1-28(20(30)31-2)15-16(22)25-18(26-17(15)23)14-12-7-5-9-24-19(12)29(27-14)10-11-6-3-4-8-13(11)21/h3-9H,10H2,1-2H3,(H4,22,23,25,26)
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Chemical Name |
methyl N-[4,6-diamino-2-[1-[(2-fluorophenyl)methyl]pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl]-N-methylcarbamate
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Synonyms |
Riociguat; BAY 63-2521; BAY63-2521; BAY632521; Trade name: Adempas
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.92 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.92 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT02117791 | Active Recruiting |
Drug: Riociguat (ADEMPAS, BAY63-2521) |
Hypertension, Pulmonary | Bayer | July 16, 2014 | N/A |
NCT02562235 | Active Recruiting |
Drug: Riociguat (Adempas, BAY63-2521) |
Hypertension, Pulmonary | Bayer | October 29, 2015 | Phase 3 |
NCT01065454 | Active Recruiting |
Drug: Riociguat (Adempas, BAY63-2521) Drug: Placebo |
Hypertension, Pulmonary Ventricular Dysfunction, Left |
Bayer | April 14, 2010 | Phase 2 |
NCT00694850 | Active Recruiting |
Drug: Riociguat (Adempas, BAY63-2521) |
Hypertension, Pulmonary | Bayer | August 2, 2008 | Phase 2 |
NCT02759419 | Recruiting | Drug: Adempas (Riociguat, BAY63-2521) |
Hypertension, Pulmonary | Bayer | June 16, 2016 | Phase 4 |
Riociguat prevents hyperoxia-ablated vascular development.PLoS One. 2018 Jul 10;13(7):e0199927. th> |
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Riociguat decreases hyperoxia-induced vascular remodeling.PLoS One. 2018 Jul 10;13(7):e0199927. td> |
Riociguat reduces and alters hyperoxia-induced lung inflammation.PLoS One. 2018 Jul 10;13(7):e0199927. td> |