Bosentan

Catalog No.S4220 Batch:S422001

Technical Data

Formula

C₂₇H₂₉N₅O₆S

Molecular Weight

551.61

CAS No.

147536-97-8

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (181.28 mM)

Ethanol

3 mg/mL (5.43 mM)

Water

Insoluble

In Vivo (Add solvents to the product individually and in order.)

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with K_i of 4.7 nM and 95 nM, respectively.

Targets

ET-A	ET-B
4.7 nM(Ki)	95 nM(Ki)

In vitro

In vitro, bosentan has been shown to improve human endothelial cell and reduce neointimal and smooth muscle proliferation.

In Vivo

In pigs in vivo, bosentan has been shown to partially restore hypoxia-induced reductions in nitric oxide.

Protocol (from reference)

Cell Assay:^{^[4]}	Cell Lines Human Hepatocytes Concentrations 1, 10 and 100 µM Incubation Time 24 h Method 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.
Animal Study:^{^[2]}	Animal Models DSS rats, Wistar rats Dosages 3 to 600 mg/kg Administration oral administration

Cell Assay:^{^[4]}

Cell Lines
Human Hepatocytes
Concentrations
1, 10 and 100 µM
Incubation Time
24 h
Method
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.

Animal Study:^{^[2]}

Animal Models
DSS rats, Wistar rats
Dosages
3 to 600 mg/kg
Administration
oral administration

References

https://pubmed.ncbi.nlm.nih.gov/19791841/
https://pubmed.ncbi.nlm.nih.gov/24582812/
https://pubmed.ncbi.nlm.nih.gov/21119207/

https://pubmed.ncbi.nlm.nih.gov/24498134/

Expand

Customer Product Validation

: Data from [ , , PLoS One, 2016, 11(9): e0161988. ]

Sellecks Bosentan Has Been Cited by 2 Publications

Acquired resistance to combination treatment through loss of synergy with MEK and PI3K inhibitors in colorectal cancer. [Bhattacharya B, et al. Oncotarget, 2016, 7(20):29187-98]	PubMed: 27081080
Stimulation of Transforming Growth Factor-β1-Induced Endothelial-To-Mesenchymal Transition and Tissue Fibrosis by Endothelin-1 (ET-1): A Novel Profibrotic Effect of ET-1 [Wermuth PJ, et al. PLoS One, 2016, 11(9):e0161988]	PubMed: 27583804

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.