1. GPCR/G Protein
  2. Endothelin Receptor
  3. Ambrisentan

Ambrisentan (Synonyms: BSF 208075; LU 208075)

Cat. No.: HY-13209 Purity: 99.86%
Handling Instructions

Ambrisentan is a selective ET type A receptor (ETAR) antagonist.

For research use only. We do not sell to patients.

Ambrisentan Chemical Structure

Ambrisentan Chemical Structure

CAS No. : 177036-94-1

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10 mM * 1 mL in DMSO USD 66 In-stock
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100 mg USD 348 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Ambrisentan is a selective ET type A receptor (ETAR) antagonist.

IC50 & Target

ETA receptor[1]

In Vitro

Ambrisentan is an endothelin type A receptor antagonist[1]. 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[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 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[1].

Clinical Trial
Molecular Weight

378.42

Formula

C₂₂H₂₂N₂O₄

CAS No.

177036-94-1

SMILES

O=C([[email protected]](C(OC)(C1=CC=CC=C1)C2=CC=CC=C2)OC3=NC(C)=CC(C)=N3)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (264.26 mM; Need ultrasonic)

Ethanol : 7.14 mg/mL (18.87 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6426 mL 13.2128 mL 26.4257 mL
5 mM 0.5285 mL 2.6426 mL 5.2851 mL
10 mM 0.2643 mL 1.3213 mL 2.6426 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.61 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.61 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.71 mg/mL (1.88 mM); Clear solution

  • 4.

    Add each solvent one by one:  10% EtOH    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.71 mg/mL (1.88 mM); Clear solution

  • 5.

    Add each solvent one by one:  10% EtOH    90% corn oil

    Solubility: ≥ 0.71 mg/mL (1.88 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
A total of 13 male FLS-ob/ob mice (age, 8 wk; body weight, 42.88 g±1.74 g) are used. At the age of 12 wk, male FLS-ob/ob mice are randomly assigned to the Ambrisentan (n=8) or control (n= 5) group. Intragastric gavage administration is carried out in conscious animals with an appropriately sized gastric tube. Ambrisentan (2.5 mg/kg per day) is orally administered every afternoon for 4 wk as a bolus through a gastric tube. Water is administered to the control group. At week 4, animals are fasted for 4 h and tail vein blood is drawn and subjected to blood glucose determination. Animals are killed by pentobarbital anesthesia injection after 4 wk and blood is collected from the right ventricle. Plasma samples are frozen and stored at -80°C Liver and visceral fat are then weighed, snap-frozen in liquid nitrogen, and stored at -80°C. Additional liver specimens are fixed in 10% buffered formalin and embedded in paraffin for histological analysis.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

AmbrisentanBSF 208075LU 208075BSF208075BSF-208075LU208075LU-208075Endothelin ReceptorInhibitorinhibitorinhibit

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Ambrisentan
Cat. No.:
HY-13209
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