product name Riociguat (BAY 63-2521)
Description: Riociguat (also known as BAY 63-2521; BAY 632521) is a novel, oral soluble guanylate cyclase (GC) stimulator, it is used in the treatment of ipulmonary hypertension. Riociguat is currently in clinical development by Bayer. The Phase III clinical trials investigated 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.
References: Eur Respir J. 2008 Oct;32(4):881-91; Br J Pharmacol. 2015 Nov;172(21):5199-210.
Formula
CAS No.
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO:
Water: <1 mg/mL
Ethanol:
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: BAY 63-2521 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. Riociguat inhibits platelet function in washed platelets but not in whole blood, and exerts no direct effects on contractility and relaxation of cardiac myocytes. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In chronic treatment of hypoxic mice and MCT-injected rats, 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. |
| Animal model | Chronic hypoxic mice, and monocrotaline (MCT)-injected rats |
| Formulation & Dosage | Dissolved in 2% methylcellulose solution; 10 mg/kg; Oral gavage |
| References | Eur Respir J. 2008 Oct;32(4):881-91; Br J Pharmacol. 2015 Nov;172(21):5199-210. |
