1386915-48-5
1386915-48-5 structure
- Name: Ambrisentan sodium
- Chemical Name: Ambrisentan sodium
- CAS Number: 1386915-48-5
- Molecular Formula: C22H21N2NaO4
- Molecular Weight: 400.40
- Catalog: Signaling Pathways GPCR/G Protein Endothelin Receptor
- Create Date: 2022-08-06 10:28:01
- Modify Date: 2025-08-21 15:16:30
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Ambrisentan (BSF 208075) sodium is a selective and orally active ET type A receptor (ETAR) antagonist[1][2].
| Name | Ambrisentan sodium |
|---|
| Description | Ambrisentan (BSF 208075) sodium is a selective and orally active ET type A receptor (ETAR) antagonist[1][2]. |
|---|---|
| Related Catalog | |
| Target |
ETA receptor[1] |
| In Vitro | Ambrisentan sodium is an endothelin type A receptor antagonist[1]. Ambrisentan sodium induces Nrf2 activation. Endothelial permeability increased in BMEC monolayers at 24 h of hypoxia exposure and compared to vehicle control, Ambrisentan attenuates hypoxia-induced BMEC leak. These results are reversed when prior to treatment BMEC are transfected with siRNA against Nrf2[2]. |
| In Vivo | In the Ambrisentan group, hepatic hydroxyproline content is significantly lower than in the control group (18.0 μg/g±6.1 μg/g vs 33.9 μg/g±13.5 μg/g liver, respectively, P=0.014). Hepatic fibrosis estimated by Sirius red staining and areas positive for α-smooth muscle actin, indicative of activated hepatic stellate cells, are also significantly lower in the Ambrisentan group (0.46%±0.18% vs 1.11%±0.28%, respectively, P=0.0003; and 0.12%±0.08% vs 0.25%±0.11%, respectively, P=0.047). Moreover, hepatic RNA expression levels of procollagen-1 and tissue inhibitor of metalloproteinase-1 (TIMP-1) are significantly lower by 60% and 45%, respectively, in the Ambrisentan group. Inflammation, steatosis, and endothelin-related mRNA expression in the liver are not significantly different between the groups. Ambrisentan sodium attenuates the progression of hepatic fibrosis by inhibiting hepatic stellate cell activation and reducing procollagen-1 and TIMP-1 gene expression. Ambrisentan sodium did not affect inflammation or steatosis[1]. |
| References |
| Molecular Formula | C22H21N2NaO4 |
|---|---|
| Molecular Weight | 400.40 |