Ambrisentan | 安倍生坦 | MedChemExpress (MCE)
品牌 | 厂商性质 | 产地 | 货期 | 价格 |
---|---|---|---|---|
MedChemExpress (MCE) | 生产商 | 美国 | 现货 | 550 |
性能特点
Ambrisentan 是一种选择性的ET A型受体 (ETAR) 拮抗剂。
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
10 mM * 1 mL | 177036-94-1 | ¥550.00 | 询底价 |
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Ambrisentan
CAS No. : 177036-94-1
MCE 国际站:Ambrisentan
产品活性:Ambrisentan 是一种选择性的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 is an endothelin type A receptor antagonist. Ambrisentan 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 attenuates the progression of hepatic fibrosis by inhibiting hepatic stellate cell activation and reducing procollagen-1 and TIMP-1 gene expression. Ambrisentan did not affect inflammation or steatosis.
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