Ambrisentan

Synonyms: LU-208075, BSF-208075

Ambrisentan (LU-208075, BSF-208075) is a highly selective antagonist of the endothelin-1 type A receptor, used in the treatment of pulmonary arterial hypertension (PAH).

Ambrisentan Chemical Structure

Ambrisentan Chemical Structure

CAS: 177036-94-1

Selleck's Ambrisentan has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.98%
99.98

Ambrisentan Related Products

Choose Selective Endothelin Receptor Inhibitors

Biological Activity

Description Ambrisentan (LU-208075, BSF-208075) is a highly selective antagonist of the endothelin-1 type A receptor, used in the treatment of pulmonary arterial hypertension (PAH).
Targets
ET-A [1]
In vitro
In vitro Ambrisentan only increases intracellular calcein fluorescence in P388/dx cells at concentrations above 100 μM and in L-MDR1 cells not at all indicating negligible P-gp inhibition. [1] Ambrisentan inhibits specific [(125)I]ET-1 binding in these tissues in a concentration-dependent manner. [2] Ambrisentan undergoes oxidative metabolism mainly by cytochrome P450 (CYP) 3A4 and to a lesser extent by CYP3A5 and CYP2C19. Ambrisentan is not only a strong inducer of CYP3A4, but also of ABCB1 and ABCG2. Ambrisentan also has a concentration-dependent effect on PXR activity, but because plateau effects are not reached, an EC50-value could not be calculated. [3] Ambrisentan inhibits specific [(125)I]ET-1 binding in a concentration-dependent manner at nanomolar ranges of IC50. Ambrisentan significantly increases the dissociation constant for bladder [(125)I]ET-1 binding without affecting maximal number of binding sites (Bmax). Ambrisentan seem to bind to bladder ET-1 receptor in a competitive and reversible manner. [4] Ambrisentan is an effective and safe treatment which is a valuable addition to the armamentarium against PAH. Ambrisentan offers a relative lack of drug interactions, once daily dosing and reassuring liver safety, offering safety and convenience advantages over bosentan. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02712346 Completed
Sickle Cell Anemia
Augusta University|Gilead Sciences|National Heart Lung and Blood Institute (NHLBI)
September 2015 Phase 1
NCT02080637 Completed
Hypoplastic Left Heart Syndrome|Hypoplastic Right-sided Heart Complex
Kevin Hill|Duke University
July 2015 Phase 2
NCT01894022 Terminated
Hypertension
GlaxoSmithKline
January 23 2014 Phase 3

Chemical Information & Solubility

Molecular Weight 378.42 Formula

C22H22N2O4

CAS No. 177036-94-1 SDF Download Ambrisentan SDF
Smiles CC1=CC(=NC(=N1)OC(C(=O)O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 75 mg/mL ( (198.19 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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