Ambrisentan

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

Ambrisentan Chemical Structure

Molecular Weight(MW): 378.42

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

Size Price Stock Quantity  
In DMSO USD 220 In stock
USD 170 In stock
USD 570 In stock
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Biological Activity

Description Ambrisentan 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

Solubility (25°C)

In vitro DMSO 76 mg/mL (200.83 mM)
Ethanol 22 mg/mL (58.13 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 378.42
Formula

C22H22N2O4

CAS No. 177036-94-1
Storage powder
Synonyms LU-208075,BSF-208075

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02885012 Recruiting Pulmonary Arterial Hypertension Medical University of South Carolina|Ochsner Health System June 2016 Phase 4
NCT02688387 Recruiting Hypertension, Pulmonary GlaxoSmithKline|Covance Harrogate|Hammersmith Medicines Research March 2016 Phase 1
NCT02253394 Recruiting Pulmonary Arterial Hypertension Brigham and Womens Hospital|Gilead Sciences September 2015 Phase 4
NCT02712346 Recruiting Sickle Cell Anemia Augusta University|Gilead Sciences|National Heart, Lung, and Blood Institute (NHLBI) September 2015 Phase 1
NCT02080637 Recruiting Hypoplastic Left Heart Syndrome|Hypoplastic Right-sided Heart Complex Kevin Hill|Duke University July 2015 Phase 2
NCT02290613 Unknown status Systemic Sclerosis|Pulmonary Hypertension Heidelberg University|GlaxoSmithKline December 2014 Phase 2

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Endothelin Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID