Bosentan

SKU: orb1300924

Description

Bosentan is a competitive sulfonamide-derived endothelin receptor antagonist with a preference for the ETA receptor. It inhibits the potent vasoconstrictor endothelin-1, reducing vascular resistance. It is widely used in pulmonary hypertension research and has been applied in both in vitro receptor binding assays and in vivo animal models of cardiovascular disease.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 147536-97-8
• MW: 551.614
• Purity: >99.99% (May vary between batches)
• Formula: C₂₇H₂₉N₅O₆S
• SMILES: COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(cc2)C(C)(C)C)nc(nc1OCCO)-c1ncccn1
• Target: Endothelin Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.63 mM);DMSO:245 mg/mL (444.15 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:3 mg/mL (5.44 mM)

Bioactivity

• Target IC50:
  ETA:4.7 nM(Ki)|ETB:95 nM(Ki)
• In Vivo:
  In pigs in vivo, bosentan has been shown to partially restore hypoxia-induced reductions in nitric oxide.
• In Vitro:
  In vitro, bosentan has been shown to improve human endothelial cell and reduce neointimal and smooth muscle proliferation.
• Cell Research:
  Incubation solutions containing bosentan (1, 10 and 100 µM) are prepared in cell culture medium. On the sixth day of culturing of the sandwich-cultured hepatocytes, cell culture medium is removed from the wells and incubation solution containing bosentan is added to the cells. The cells were incubated with the solution for 24 h at 37°C. After the exposure, the incubation solution id removed and the cells are rinsed with Plus (+) or Minus (−) buffer. The buffer solution is then removed and the cells are incubated with fresh Plus (+) or Minus (−) buffer for 5 min at 37°C. Following this 5 minute incubation, the buffer solution is collected and any remaining buffer is removed. The cells are then washed three times with ice-cold Plus (+) buffer and the plates are frozen at −80°C until processed for bioanalysis. (Only for Reference)

Storage & Handling

• Storage: store at low temperature | 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

Benzenesulfonamide, Actelion, Bosentan, inhibit, Inhibitor, ET-A, ET-B, EndothelinReceptor, Endothelin Receptor, Ro 47-0203

Compound Identifiers

PubChem CID

104865