Riociguat
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MedKoo CAT#: 503750

CAS#: 625115-55-1

Description: Riociguat, also known as BAY 63-2521, is a novel drug that is currently in clinical development by Bayer. It is a stimulator of soluble guanylate cyclase (sGC). At the moment Phase III clinical trials investigate the use of riociguat as a new approach to treat two forms of pulmonary hypertension (PH): chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH). Riociguat constitutes the first drug of a novel class of sGC stimulators.


Chemical Structure

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Riociguat
CAS# 625115-55-1

Theoretical Analysis

MedKoo Cat#: 503750
Name: Riociguat
CAS#: 625115-55-1
Chemical Formula: C20H19FN8O2
Exact Mass: 422.1615
Molecular Weight: 422.42
Elemental Analysis: C, 56.87; H, 4.53; F, 4.50; N, 26.53; O, 7.58

Size Price Shipping out time Quantity
25mg USD 150 Same day
50mg USD 250 Same day
100mg USD 450 Same day
200mg USD 650 Same day
500mg USD 850 Same day
1g USD 1450 Same day
5g USD 4650 2 Weeks
10g USD 5950 2 Weeks
50g USD 12850 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-03-01. Prices are subject to change without notice.

Riociguat, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 2g may be 2 weeks.

Synonym: BAY 63-2521; BAY63-2521; BAY632521; Riociguat; Brand name: Adempas.

IUPAC/Chemical Name: methyl (4,6-diamino-2-(1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)pyrimidin-5-yl)(methyl)carbamate

InChi Key: WXXSNCNJFUAIDG-UHFFFAOYSA-N

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)

SMILES Code: O=C(OC)N(C1=C(N)N=C(C2=NN(CC3=CC=CC=C3F)C4=NC=CC=C42)N=C1N)C

Appearance:
Light yellow solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 422.42 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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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.

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.

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.

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.

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.

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.

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.

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.

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.

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.



Additional Information