Soluble guanylate cyclase (sGC) stimulator
CAS:625115-55-1
分子式:C20H19FN8O2
分子量:422.42
纯度:98%
存储:Store at -20°C
Background:
Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension.
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].
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].
Reference:
[1]. Schermuly RT, et al. Expression and function of soluble guanylate cyclase in pulmonary arterial hypertension. Eur Respir J. 2008 Oct;32(4):881-91.
[2]. Schermuly RT, et al. Riociguat for the treatment of pulmonary hypertension. Expert Opin Investig Drugs. 2011 Apr;20(4):567-76.
[3]. Donda K, et al. Riociguat prevents hyperoxia-induced lung injury and pulmonary hypertension in neonatal rats without effects on long bone growth. PLoS One. 2018 Jul 10;13(7):e0199927.