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Ambrisentan

Catalog No. T1655   CAS 177036-94-1
Synonyms: BSF-208075, BSF 208075, LU 208075

Ambrisentan (BSF 208075) is an endothelin receptor antagonist used in the therapy of pulmonary arterial hypertension (PAH). Ambrisentan has been associated with a low rate of serum enzyme elevations during therapy but has yet to be implicated in cases of clinically apparent acute liver injury.

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Ambrisentan Chemical Structure
Ambrisentan, CAS 177036-94-1
Pack Size Availability Price/USD Quantity
5 mg In stock $ 50.00
10 mg In stock $ 63.00
25 mg In stock $ 117.00
50 mg In stock $ 178.00
100 mg In stock $ 265.00
500 mg In stock $ 657.00
1 mL * 10 mM (in DMSO) In stock $ 58.00
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Purity: 99.85%
Purity: 99.65%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ambrisentan (BSF 208075) is an endothelin receptor antagonist used in the therapy of pulmonary arterial hypertension (PAH). Ambrisentan has been associated with a low rate of serum enzyme elevations during therapy but has yet to be implicated in cases of clinically apparent acute liver injury.
In vivo In the Ambrisentan group, hepatic hydroxyproline content was significantly reduced (18.0 μg/g±6.1 vs. 33.9 μg/g±13.5 in the control group, P=0.014), indicating a lower level of hepatic fibrosis. This was supported by Sirius red staining and α-smooth muscle actin positivity, which were both significantly lower 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), suggesting reduced activation of hepatic stellate cells. Furthermore, RNA expression levels of procollagen-1 and TIMP-1 in the liver were significantly decreased by 60% and 45%, respectively, in the Ambrisentan group, further demonstrating its effectiveness in attenuating hepatic fibrosis. However, Ambrisentan did not significantly impact inflammation, steatosis, or endothelin-related mRNA expression in the liver. This evidence supports that Ambrisentan hinders the progression of hepatic fibrosis by suppressing hepatic stellate cell activation and diminishing procollagen-1 and TIMP-1 gene expression, without affecting inflammation or steatosis.
Kinase Assay In vitro PTPase assays: Individual PTPases (0.01 μg/reaction) in 50 μL of PTPase buffer [50 mM Tris (pH 7.4)] are incubated at 22 ℃ for 10 min or as indicated in the absence or presence of inhibitory compounds. Substrates (0.2 mM phosphotyrosine peptide) are then added and allows to react at 22 ℃ for 18 hr. PTPase activity of individual reactions is measured by adding 100 μL of malachite green solution (UBI) and then quantifying the amounts of free phosphate cleaved by the PTPase from the peptide substrate by spectrometry (A660 nm). Relative PTPase activities are calculated based on the formula [(PTPase activity in the presence of an inhibitory compound)/(PTPase activity in the absence of the compound) &times 100%]. Reactions performed under comparable conditions in the absence of recombinant PTPases only are used as controls and shows no detectable PTPase activity.
Cell Research Ambrisentan is dissolved in DMSO and stored, and then diluted with appropriate medium before use. Unless otherwise stated, for each BMEC experiment cells are randomly divided into 4 groups: (1) normoxia vehicle control (Nx-CTRL); (2) normoxia-treated; (3) hypoxia (24 h) control (Hx-CTRL) and (4) hypoxia (24 h) treated. As previously described, Nrf2 activators are added 24 h prior to any hypoxic exposures. Cell treatments are; Protandim (100 μg/mL), methazolamide (125 μg/mL, nifedipine (7 μg/mL) or Ambrisentan (40 μg/mL). In addition, some cells are treated with Nrf2 siRNA. In these experiments, siRNA is added 24 h prior to drug treatments. The rationale for 24 h hypoxia exposure for BMEC is to ensure that cells remained transfected with siRNA for the pre-treatment of drugs (24 h in normoxia) and during the 24 h hypoxia exposure. Data is collected from at least three separate cell culture preparations on three separate days (n=9)[2].
Synonyms BSF-208075, BSF 208075, LU 208075
Molecular Weight 378.42
Formula C22H22N2O4
CAS No. 177036-94-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 6 mg/mL(15.9 mM)

DMSO: 71 mg/mL (187.6 mM)

TargetMolReferences and Literature

1. Weiss J, et al. Eur J Pharmacol,2011, 660(2-3), 298-304. 2. Yokoyama Y, et al. Biol Pharm Bull,2014, 37(3), 461-465. 3. Weiss J, et al. Biochem Pharmacol,2013, 85(2), 265-273. 4. Osano A, et al. J Pharmacol Sci,2014, 124(1), 86-91. 5. Buckley MS, et al. Expert Opin Drug Metab Toxicol,2011, 7(3), 371-380. 6. 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.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cardiovascular Disease Compound Library Anti-Cancer Compound Library FDA-Approved & Pharmacopeia Drug Library Endocrinology-Hormone Compound Library Neurotransmitter Receptor Compound Library Inhibitor Library

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Keywords

Ambrisentan 177036-94-1 GPCR/G Protein Endothelin Receptor inhibit BSF-208075 BSF 208075 LU-208075 BSF208075 Inhibitor LU208075 LU 208075 inhibitor

 

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