Ambrisentan sodium

Modify Date: 2024-01-16 17:13:12

Ambrisentan sodium structure	Common Name	Ambrisentan sodium
	CAS Number	1386915-48-5	Molecular Weight	400.40
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₂H₂₁N₂NaO₄	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Ambrisentan sodium

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	Research Areas >> Cardiovascular Disease Research Areas >> Endocrinology Signaling Pathways >> GPCR/G Protein >> Endothelin Receptor
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	[1]. Okamoto T, et al. Antifibrotic effects of Ambrisentan, an endothelin-A receptor antagonist, in a non-alcoholic steatohepatitis mouse model. World J Hepatol. 2016 Aug 8;8(22):933-41. [2]. Lisk C, et al. Nrf2 activation: a potential strategy for the prevention of acute mountain sickness. Free Radic Biol Med. 2013 Oct;63:264-73.

Molecular Formula	C₂₂H₂₁N₂NaO₄
Molecular Weight	400.40