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Cat. No.: HY-13209C

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Ambrisentan sodium

(Synonyms: BSF 208075 sodium; LU 208075 sodium)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

Ambrisentan (BSF 208075) sodium is a selective and orally active ET type A receptor (ETAR) antagonist.

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

CAS No.: 1386915-48-5
Formula: C₂₂H₂₁N₂NaO₄
Molecular Weight:400.40

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (278 KB)

Ambrisentan sodium Chemical Structure

CAS No.: 1386915-48-5

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Top Publications Citing

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Publications Citing Use of MedChemExpress (MCE) Ambrisentan sodium

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RT-PCRWBIn Vivo Efficacy StudyHistological Imaging/Staining

RT-PCR
WB
In Vivo Efficacy Study
Histological Imaging/Staining
In Vivo Efficacy Study

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

Ambrisentan (BSF 208075) sodium is a selective and orally active ET type A receptor (ETAR) antagonist^[1]^[2].

IC₅₀ & Target

ET_A

All Endothelin Receptor Isoforms :

ET_A
ET_B

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].

MedChemExpress (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 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].

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

Chemical Information

CAS No. 1386915-48-5
Molecular Weight 400.40
Formula C₂₂H₂₁N₂NaO₄
SMILES

O=C(O[Na])[C@@H](OC1=NC(C)=CC(C)=N1)C(C2=CC=CC=C2)(OC)C3=CC=CC=C3
Synonyms

BSF 208075 sodium; LU 208075 sodium
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (2)

All RT-PCRWBIn Vivo Efficacy StudyHistological Imaging/Staining

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J Mol Cell Cardiol

Induction of GLI1 by miR-27b-3p/FBXW7/KLF5 pathway contributes to pulmonary arterial hypertension. [Abstract]

2022 Oct:171:16-29. PMID: 35810662

Ambrisentan sodium purchased from MedChemExpress. Usage Cited in: J Mol Cell Cardiol. 2022 Oct:171:16-29. [Abstract]

Ambrisentan (AM; 0.2 mg/kg; PO; daily for 4 weeks) decreased the mRNA level of miR-27b-3p in lung tissues in MCT-induced PAH rats.

Ambrisentan sodium purchased from MedChemExpress. Usage Cited in: J Mol Cell Cardiol. 2022 Oct:171:16-29. [Abstract]

Ambrisentan (AM; 0.2 mg/kg; PO; daily for 4 weeks) decreased the protein level of KLF5, GLI1 in lung tissues in MCT-induced PAH rats.

Ambrisentan sodium purchased from MedChemExpress. Usage Cited in: J Mol Cell Cardiol. 2022 Oct:171:16-29. [Abstract]

Ambrisentan (AM; 0.2 mg/kg; PO; daily for 4 weeks) reduced the increase of RVSP and the elevations of RV/(LV + S) in MCT-induced PAH rats.

Ambrisentan sodium purchased from MedChemExpress. Usage Cited in: J Mol Cell Cardiol. 2022 Oct:171:16-29. [Abstract]

Ambrisentan (AM; 0.2 mg/kg; PO; daily for 4 weeks) reduced PASMC proliferation of pulmonary arterioles in MCT-induced PAH rats.

Ambrisentan sodium purchased from MedChemExpress. Usage Cited in: J Mol Cell Cardiol. 2022 Oct:171:16-29. [Abstract]

Ambrisentan (AM; 0.2 mg/kg; PO; daily for 4 weeks) reduced pulmonary arterioles medial wall thickness, proportion of muscularized arteries in MCT-induced PAH rats.
Patent

US20220317132A1.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Ambrisentan sodium

2 Cited Publications

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Purity & Documentation
References

1/16
1/16

Ambrisentan sodium purchased from MedChemExpress. Usage Cited in: J Mol Cell Cardiol. 2022 Oct:171:16-29. [Abstract]

Customer Validation
Ambrisentan (AM; 0.2 mg/kg; PO; daily for 4 weeks) decreased the mRNA level of miR-27b-3p in lung tissues in MCT-induced PAH rats.
1/16

Ambrisentan sodium purchased from MedChemExpress. Usage Cited in: J Mol Cell Cardiol. 2022 Oct:171:16-29. [Abstract]

Customer Validation
Ambrisentan (AM; 0.2 mg/kg; PO; daily for 4 weeks) decreased the protein level of KLF5, GLI1 in lung tissues in MCT-induced PAH rats.
1/16

Ambrisentan sodium purchased from MedChemExpress. Usage Cited in: J Mol Cell Cardiol. 2022 Oct:171:16-29. [Abstract]

Customer Validation
Ambrisentan (AM; 0.2 mg/kg; PO; daily for 4 weeks) reduced the increase of RVSP and the elevations of RV/(LV + S) in MCT-induced PAH rats.
1/16

Ambrisentan sodium purchased from MedChemExpress. Usage Cited in: J Mol Cell Cardiol. 2022 Oct:171:16-29. [Abstract]

Customer Validation
Ambrisentan (AM; 0.2 mg/kg; PO; daily for 4 weeks) reduced PASMC proliferation of pulmonary arterioles in MCT-induced PAH rats.
1/16

Ambrisentan sodium purchased from MedChemExpress. Usage Cited in: J Mol Cell Cardiol. 2022 Oct:171:16-29. [Abstract]

Customer Validation
Ambrisentan (AM; 0.2 mg/kg; PO; daily for 4 weeks) reduced pulmonary arterioles medial wall thickness, proportion of muscularized arteries in MCT-induced PAH rats.

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Ambrisentan sodium

Publications Citing Use of MedChemExpress (MCE) Ambrisentan sodium

All Endothelin Receptor Isoforms

Biological Activity

Chemical Information

Publications (2)

Purity & Documentation

References

Calculators

Help & FAQs

Ambrisentan sodium Related Classifications

HY-13209C Related Classifications

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