Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ambrosentan (BSF 208075) sodium is a selective and oral effective antagonist of ET type A receptor ( ETAR ).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,520.00 | |
50 mg | 6-8 weeks | $ 1,980.00 | |
100 mg | 6-8 weeks | $ 2,500.00 |
Description | Ambrosentan (BSF 208075) sodium is a selective and oral effective antagonist of ET type A receptor ( ETAR ). |
In vitro | Ambrisentan sodium, an endothelin type A receptor antagonist [1], promotes Nrf2 activation. It mitigates the increase in endothelial permeability observed in BMEC monolayers after 24 hours of hypoxia, compared to a vehicle control. However, this protective effect of Ambrisentan is negated when BMEC are pre-treated with siRNA targeting Nrf2 [2]. |
In vivo | In the study, Ambrisentan treatment resulted in a notably lower hepatic hydroxyproline content compared to the control (18.0 μg/g±6.1 μg/g vs 33.9 μg/g±13.5 μg/g liver, P=0.014). Furthermore, assessments of hepatic fibrosis using Sirius red staining and the evaluation of areas positive for α-smooth muscle actin—a marker of hepatic stellate cell activation—revealed significant reductions in the Ambrisentan group (0.46%±0.18% vs 1.11%±0.28%, P=0.0003; and 0.12%±0.08% vs 0.25%±0.11%, P=0.047, respectively). Additionally, hepatic RNA expression levels of procollagen-1 and tissue inhibitor of metalloproteinase-1 (TIMP-1) were reduced by 60% and 45%, respectively, in the Ambrisentan-treated group. It's important to note that Ambrisentan sodium's effect on inflammation, steatosis, and endothelin-related mRNA expression in the liver was not significant between groups. The findings suggest that Ambrisentan sodium mitigates hepatic fibrosis progression through the inhibition of hepatic stellate cell activation and a decrease in procollagen-1 and TIMP-1 gene expression, without influencing inflammation or steatosis. |
Molecular Weight | 400.41 |
Formula | C22H21N2NaO4 |
CAS No. | 1386915-48-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Ambrisentan sodium 1386915-48-5 inhibitor inhibit