Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
10 mg | In stock | $ 32.00 | |
25 mg | In stock | $ 51.00 | |
50 mg | In stock | $ 74.00 | |
100 mg | In stock | $ 129.00 | |
200 mg | In stock | $ 217.00 | |
500 mg | In stock | $ 327.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 81.00 |
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. |
Targets&IC50 | ETB:95 nM(Ki), ETA:4.7 nM(Ki) |
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]. |
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) |
Synonyms | Actelion, Ro 47-0203, Benzenesulfonamide |
Molecular Weight | 551.614 |
Formula | C27H29N5O6S |
CAS No. | 147536-97-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 3 mg/mL (5.43 mM)
DMSO: 100 mg/mL (181.28 mM)
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Bosentan 147536-97-8 GPCR/G Protein Endothelin Receptor Actelion Ro 47-0203 Inhibitor inhibit Benzenesulfonamide inhibitor