Ambrisentan

Catalog No.S2097 Synonyms: LU-208075, BSF-208075

For research use only.

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

CAS No. 177036-94-1

Selleck's Ambrisentan has been cited by 2 Publications

Purity & Quality Control

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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

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]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 378.42
Formula

C22H22N2O4

CAS No. 177036-94-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=NC(=N1)OC(C(=O)O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)C

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02712346 Completed Drug: Ambrisentan|Drug: Placebo Sickle Cell Anemia Augusta University|Gilead Sciences|National Heart Lung and Blood Institute (NHLBI) September 2015 Phase 1
NCT02080637 Completed Drug: Ambrisentan|Other: Placebo Hypoplastic Left Heart Syndrome|Hypoplastic Right-sided Heart Complex Kevin Hill|Duke University July 2015 Phase 2
NCT01894022 Terminated Drug: Ambrisentan 5 mg Hypertension GlaxoSmithKline January 23 2014 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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