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Ambrisentan sodium

CAS No. : 1386915-48-5

MCE 国际站：Ambrisentan sodium

产品活性：Ambrisentan (BSF 208075) sodium 是一种选择性的、具有口服活性的 ET A 型受体 (ETAR) 拮抗剂。

研究领域：GPCR/G Protein

作用靶点：Endothelin Receptor

In Vitro: Ambrisentan sodium is an endothelin type A receptor antagonist.
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.

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.

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