Home GPCR & G Protein Endothelin Receptor antagonist Ambrisentan For research use only.

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

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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
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 lnformation & 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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