Riociguat

SKU: orb1221944

Description

Riociguat, also known as BAY 63-2521, is a novel drug that is currently in clinical development by Bayer. It is a stimulator of soluble guanylate cyclase (sGC). At the moment Phase III clinical trials investigate 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.(In Vitro):[3H]Rauwolscine binding to α2 adrenergic receptor is reversible, stcreospccific, and saturable. [3H]Rauwolscine specifically labels both the high and low affinity states of the α2 adrenergic receptor in brain membranes. [3H]Rauwolscine also behaves as a 5-HT1A receptor agonist and this conclusion is compatible with earlier functional studies, indicating that rauwolscine (as well as yohimbine) has agonistic properties at the level of 5-HT autoreceptors. When using [3H]5-HT as a radioligand, rauwolscine is determined to have relatively high affinity for the human receptor (Ki human=14.3 nM, Ki rat=35.8 nM). Saturation studies shows that the affinity of [3H]Rauwolscine is similar in mouse, rat, rabbit, dog (2.33-3.03 nM) except man where it is significantly higher (0.98 nM) .

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 625115-55-1
• MW: 422.42
• Purity: >98% (HPLC)
• Formula: C₂₀H₁₉FN₈O₂
• SMILES: C(=O)(N(C)c1c(nc(nc1N)c1c2c(nccc2)n(n1)Cc1c(cccc1)F)N)OC
• Target: Guanylate cyclase
• Solubility: DMSO : ≥ 50 mg/mL; 118.37 mM

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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. Riociguat inhibits platelet function in washed platelets but not in whole blood, and exerts no direct effects on contractility and relaxation of cardiac myocytes.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BAY 63-2521 | BAY63-2521 | Riociguat

Quick Database Links

Gene Symbol

Guanylate cyclase