Name: Ambrisentan
Brand: Selleck Chemicals
SKU: S2097
Availability: InStock
Rating: 5 (2 reviews)

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Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other Endothelin Receptor Inhibitors	BQ-123 Zibotentan (ZD4054) Sparsentan (PS-433540, RE-021) Lu-135252 Pearl Extract Carperitide Acetate Atrasentan Aprocitentan

Solubility

In vitro
Batch:

DMSO : 75 mg/mL (198.19 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.750mg/ml (9.91mM)	Taking the 1 mL working solution as an example, add 50 μL of 75 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.625mg/ml (1.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	378.42	Formula	C₂₂H₂₂N₂O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	177036-94-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LU-208075, BSF-208075			SMILES	CC1=CC(=NC(=N1)OC(C(=O)O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)C

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	ET-A
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. This compound inhibits specific [(125)I]ET-1 binding in these tissues in a concentration-dependent manner. It undergoes oxidative metabolism mainly by cytochrome P450 (CYP) 3A4 and to a lesser extent by CYP3A5 and CYP2C19. It is not only a strong inducer of CYP3A4, but also of ABCB1 and ABCG2. This chemical also has a concentration-dependent effect on PXR activity, but because plateau effects are not reached, an EC50-value could not be calculated. It inhibits specific [(125)I]ET-1 binding in a concentration-dependent manner at nanomolar ranges of IC50. It significantly increases the dissociation constant for bladder [(125)I]ET-1 binding without affecting maximal number of binding sites (Bmax). It seem to bind to bladder ET-1 receptor in a competitive and reversible manner. This compound is an effective and safe treatment which is a valuable addition to the armamentarium against PAH. It offers a relative lack of drug interactions, once daily dosing and reassuring liver safety, offering safety and convenience advantages over bosentan.
References	[1] https://pubmed.ncbi.nlm.nih.gov/21501604/ [2] https://pubmed.ncbi.nlm.nih.gov/24583865/ [3] https://pubmed.ncbi.nlm.nih.gov/23219525/ [4] https://pubmed.ncbi.nlm.nih.gov/24389822/ [5] https://pubmed.ncbi.nlm.nih.gov/21299444/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-05-13)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT07245680	RECRUITING	Pulmonary Arterial Hypertension (PAH); Comorbidities; Cardiovascular Disease (CVD)	Assistance Publique - Hôpitaux de Paris	2026-04-28	PHASE3
NCT06968962	RECRUITING	Pulmonary Arterial Hypertension (PAH)	Second Affiliated Hospital, Zhejiang University, School of Medicine	2025-05-14
NCT06987097	NOT_YET_RECRUITING	Pulmonary Arterial Hypertension (PAH)	Nanjing First Hospital, Nanjing Medical University	2025-05-15
NCT07030894	RECRUITING	IgA Nephropathy; Chronic Kidney Disease; Proteinuria	The First Hospital of Jilin University	2025-09-01	PHASE4
NCT06256432	ACTIVE_NOT_RECRUITING	Hepatorenal Syndrome; Liver Cirrhosis; Acute Kidney Injury; Ascites Hepatic	Noorik Biopharmaceuticals AG	2024-04-17	PHASE2
NCT04972656	UNKNOWN	Pulmonary Arterial Hypertension	Nanjing First Hospital, Nanjing Medical University	2022-09-05

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Ambrisentan Endothelin Receptor antagonist

Chemical Structure

Molecular Weight: 378.42