| Name | Bosentan |
| Description | Bosentan (Benzenesulfonamide) is a sulfonamide-derived, competitive and specific endothelin receptor antagonist with a slightly higher affinity for the endothelin A receptor than endothelin B receptor. Bosentan blocks the action of endothelin 1, an extremely potent endogenous vasoconstrictor and bronchoconstrictor, by binding to endothelin A and endothelin B receptors in the endothelium and vascular smooth muscle. Bosentan decreases both pulmonary and systemic vascular resistance and is particularly used in the treatment of pulmonary arterial hypertension. |
| 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) |
| In vitro | In vitro, bosentan has been shown to improve human endothelial cell and reduce neointimal and smooth muscle proliferation[3]. |
| In vivo | In pigs in vivo, bosentan has been shown to partially restore hypoxia-induced reductions in nitric oxide[3]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 3 mg/mL (5.43 mM)
DMSO : 55 mg/mL (99.71 mM)
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| Keywords | Bosentan | Inhibitor | inhibit | Endothelin Receptor |
| Inhibitors Related | Macitentan | BMS 182874 hydrochloride | Sulfisoxazole | Ambrisentan | Sparsentan | Aprocitentan |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
