For research use only. Not for therapeutic Use.
Riociguat (BAY 63-2521)（Cat No.:A000103）is a soluble guanylate cyclase (sGC) stimulator used to treat pulmonary arterial hypertension (PAH) and chronic thromboembolic pulmonary hypertension (CTEPH). It works by enhancing the nitric oxide (NO)-sGC-cyclic GMP pathway, leading to vasodilation and reduced pulmonary pressure. Riociguat helps improve exercise capacity and slow disease progression in PAH and CTEPH by relaxing the blood vessels in the lungs. Its dual mechanism of both directly stimulating sGC and sensitizing it to endogenous NO makes Riociguat effective in managing conditions where NO production is impaired.
| Catalog Number | A000103 |
| CAS Number | 625115-55-1 |
| Synonyms | NA |
| Molecular Formula | C20H19FN8O2 |
| Purity | ≥95% |
| Target | Guanylate Cyclase |
| Solubility | >17mg/mL in DMSO |
| Storage | Store at -20°C |
| IUPAC Name | methyl N-[4,6-diamino-2-[1-[(2-fluorophenyl)methyl]pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl]-N-methylcarbamate |
| InChI | 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) |
| InChIKey | WXXSNCNJFUAIDG-UHFFFAOYSA-N |
| SMILES | CN(C1=C(N=C(N=C1N)C2=NN(C3=C2C=CC=N3)CC4=CC=CC=C4F)N)C(=O)OC |
| Reference | </br>1: Ghio S, Bonderman D, Felix SB, Ghofrani HA, Michelakis ED, Mitrovic V, Oudiz RJ, Frey R, Roessig L, Semigran MJ. Left ventricular systolic dysfunction associated with pulmonary hypertension riociguat trial (LEPHT): rationale and design. Eur J Heart Fail. 2012 Aug;14(8):946-53. Epub 2012 Jun 20. PubMed PMID: 22719060.</br>2: Geschka S, Kretschmer A, Sharkovska Y, Evgenov OV, Lawrenz B, Hucke A, Hocher B, Stasch JP. Soluble guanylate cyclase stimulation prevents fibrotic tissue remodeling and improves survival in salt-sensitive Dahl rats. PLoS One. 2011;6(7):e21853. Epub 2011 Jul 18. PubMed PMID: 21789188; PubMed Central PMCID: PMC3138745.</br>3: Schermuly RT, Janssen W, Weissmann N, Stasch JP, Grimminger F, Ghofrani HA. Riociguat for the treatment of pulmonary hypertension. Expert Opin Investig Drugs. 2011 Apr;20(4):567-76. Epub 2011 Mar 11. Review. PubMed PMID: 21391889.</br>4: Mitrovic V, Jovanovic A, Lehinant S. Soluble guanylate cyclase modulators in heart failure. Curr Heart Fail Rep. 2011 Mar;8(1):38-44. Review. PubMed PMID: 21207207.</br>5: Kim NH. Riociguat: an upcoming therapy in chronic thromboembolic pulmonary hypertension? Eur Respir Rev. 2010 Mar;19(115):68-71. Review. PubMed PMID: 20956169.</br>6: Frey R, Mück W, Kirschbaum N, Krätzschmar J, Weimann G, Wensing G. Riociguat (BAY 63-2521) and warfarin: a pharmacodynamic and pharmacokinetic interaction study. J Clin Pharmacol. 2011 Jul;51(7):1051-60. Epub 2010 Aug 27. PubMed PMID: 20801938.</br>7: Sharkovska Y, Kalk P, Lawrenz B, Godes M, Hoffmann LS, Wellkisch K, Geschka S, Relle K, Hocher B, Stasch JP. Nitric oxide-independent stimulation of soluble guanylate cyclase reduces organ damage in experimental low-renin and high-renin models. J Hypertens. 2010 Aug;28(8):1666-75. PubMed PMID: 20613628.</br>8: Ghofrani HA, Hoeper MM, Halank M, Meyer FJ, Staehler G, Behr J, Ewert R, Weimann G, Grimminger F. Riociguat for chronic thromboembolic pulmonary hypertension and pulmonary arterial hypertension: a phase II study. Eur Respir J. 2010 Oct;36(4):792-9. Epub 2010 Jun 7. PubMed PMID: 20530034.</br>9: Schenk M. [Pulmonary arterial hypertension–a rare form of pulmonary hypertension]. Dtsch Med Wochenschr. 2010 May;135(21):p21. Epub 2010 May 27. German. PubMed PMID: 20509110.</br>10: Loukanov T, Geiger R, Agrawal R. Animal models related to congenital heart disease and clinical research in pulmonary hypertension. Cardiology. 2010;116(1):18-25. Epub 2010 Apr 24. PubMed PMID: 20424448.</br> |
