Riociguat 是一种鸟苷酸环化酶的刺激剂，可导致血管平滑肌松弛，用于治疗严重的肺动脉高压。
产品描述
Riociguat is a stimulator of guanylate cyclase which causes relaxation of vascular smooth muscle and is used to treat severe pulmonary arterial hypertension.
体外活性
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. [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] [3]
体内活性
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. [1]
Cas No.
625115-55-1
分子式
C20H19FN8O2
分子量
422.42
别名
利奥西呱;BAY 632521
储存和溶解度
DMSO:78 mg/mL (184.7 mM)
H2O:<1 mgml
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
