Riociguat

SKU: orb1300303

Description

Riociguat (BAY 632521) is a soluble guanylate cyclase (sGC) stimulator used in research for severe pulmonary arterial hypertension. It induces vasodilation by enhancing cGMP signaling and is applied in both in vitro mechanistic studies and in vivo animal models of pulmonary hypertension.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 625115-55-1
• MW: 422.42
• Purity: 99.95% (May vary between batches)
• Formula: C₂₀H₁₉FN₈O₂
• SMILES: COC(=O)N(C)c1c(N)nc(nc1N)-c1nn(Cc2ccccc2F)c2ncccc12
• Target: Guanylate cyclase
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.73 mM);DMSO:40.83 mg/mL (96.66 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• In Vivo:
  In a long-term study, Riociguat (10 mg/kg/d, orally) was found to partially mitigate pulmonary arterial hypertension, right heart hypertrophy, and structural remodeling of lung vasculature in hypoxic mice and monocrotaline (MCT)-injected rats.
• In Vitro:
  BAY 63-2521 (Riociguat) concentration-dependently stimulates the recombinant soluble guanylate cyclase (sGC) from 0.1 to 100 μM, resulting in a two-fold to 73-fold increase, through an NO-independent but haem-dependent mechanism. Additionally, Riociguat impairs platelet function in isolated platelets, though it does not affect platelets in whole blood, nor does it directly influence the contractility and relaxation of cardiac myocytes.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BAY632521, BAY-632521, BAY 632521, guanylate cyclase, Guanylatecyclase, Guanylate Cyclase, Guanylate cyclase, Inhibitor, inhibit, Riociguat

Compound Identifiers

PubChem CID

11304743