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 No. 177036-94-1

Purity & Quality Control

Ambrisentan Related Products

Signaling Pathway

Endothelin Receptor Signaling Pathways

Endothelin Receptor Signaling Pathway

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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Ambrisentan | Ambrisentan ic50 | Ambrisentan price | Ambrisentan cost | Ambrisentan solubility dmso | Ambrisentan purchase | Ambrisentan manufacturer | Ambrisentan research buy | Ambrisentan order | Ambrisentan mouse | Ambrisentan chemical structure | Ambrisentan mw | Ambrisentan molecular weight | Ambrisentan datasheet | Ambrisentan supplier | Ambrisentan in vitro | Ambrisentan cell line | Ambrisentan concentration | Ambrisentan nmr