ET receptor antagonist 1

Name: ET receptor antagonist 1
Brand: TargetMol
SKU: T79573
Rating: 4.5 (1 reviews)

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Catalog No. T79573

ET Receptor Antagonist 1 (compound 16h), with an IC50 value of 0.18 nM, is an orally active agent that can be utilized for pulmonary arterial hypertension (PAH) research. It has demonstrated efficacy in mitigating monocrotaline-induced PAH in a rat model [1].

ET receptor antagonist 1

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Catalog No. T79573

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
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50 mg	Inquiry	Inquiry	Inquiry

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Product Introduction

Bioactivity

Description	ET Receptor Antagonist 1 (compound 16h), with an IC50 value of 0.18 nM, is an orally active agent that can be utilized for pulmonary arterial hypertension (PAH) research. It has demonstrated efficacy in mitigating monocrotaline-induced PAH in a rat model [1].
In vivo	ET receptor antagonist 1 (compound 16h), administered orally at 150 mg/kg/d and 300 mg/kg/d starting 48 hours post-MCT treatment for 21-26 days, significantly reduced mean pulmonary arterial pressure (mPAP) in MCT-exposed rats, decreased HIF1α, ANP, and TNNI3 levels, and exhibited antioxidant properties while inhibiting lipid peroxidation [1].

Chemical Properties

Molecular Weight	459.52
Formula	C₂₁H₂₅N₅O₅S

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc