Riociguat , ≥99% , 625115-55-1

CAS NO.：625115-55-1

Empirical Formula: C20H19FN8O2

Molecular Weight: 422.42

MDL number: MFCD19443708

EINECS: 641-755-1

PRODUCT Properties

• Melting point: 247-251°C (dec.)
• Boiling point: 567.2±50.0 °C(Predicted)
• Density: 1.51
• storage temp.: Refrigerator
• solubility: DMSO (Slightly, Heated), Methanol (Slightly, Heated)
• pka: 1.51±0.50(Predicted)
• form: Solid
• color: Off-White to Orange
• 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: C(OC)(=O)N(C1=C(N)N=C(C2C3=CC=CN=C3N(CC3=CC=CC=C3F)N=2)N=C1N)C

Description and Uses

Riociguat is a first-in-class oral medication that adds to the treatment options for PAH. In September 2013, Health Canada approved riociguat (also referred to as BAY 63-2521), for the treatment of patients with chronic thromboembolic pulmonary hypertension (CTEPH) after surgical treatment or inoperable CTEPH and for the treatment of adults with pulmonary arterial hypertension (PAH). Riociguat has a dual mode of action and works by (a) sensitizing sGC to the body's NO by stabilizing NO–sGC binding and (b) an NO-independent, direct stimulation of sGC via a different binding site. This process restores the NO–sGC–cGMP pathway and leads to increased generation of cGMP with subsequent vasodilation.
Headache, dizziness, dyspepsia/gastritis, nausea, diarrhea, hypotension, vomiting, anemia, gastroesophageal reflux, and constipation were the most common adverse events ( 3%) observed during riociguat clinical trials. Riociguat comes with a black box warning for embryo-fetal toxicity.

Riociguat is used in the treatment for pulmonary hypertension.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302
• Precautionary statements: P264-P270-P301+P312-P330-P501