| 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 | Store at low temperature | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 3 mg/mL (5.44 mM), Sonication is recommended.
DMSO : 245 mg/mL (444.15 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.63 mM), Sonication is recommended.
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| Keywords | Inhibitor | inhibit | ET-B | ET-A | EndothelinReceptor | Endothelin Receptor | Bosentan |
| Inhibitors Related | BQ-788 | Macitentan | BMS 182874 | BMS 182874 hydrochloride | Sitaxsentan sodium | Edonentan | SB-209670 | Ambrisentan | Sparsentan | Aprocitentan | Nebentan potassium | Clazosentan |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
