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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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
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10 mg USD 72 In-stock
Estimated Time of Arrival: December 31
50 mg USD 228 In-stock
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100 mg USD 348 In-stock
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Customer Review

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].

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

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].

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

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

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Ambrisentan
Cat. No.:
HY-13209
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