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THR-β agonist 10

Catalog No. T213214 Copy Product Info
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THR-β agonist 10 is an orally active and selective THR-β agonist with an EC50 value of 11 nM. It effectively lowers levels of ALT (alanine aminotransferase), TC (total cholesterol), and LDL-C (low-density lipoprotein cholesterol). In mouse models of metabolic dysfunction-associated steatohepatitis (MASH), it improves steatosis, ballooning, inflammation, and fibrosis. THR-β agonist 10 is utilized in the research of MASH.

THR-β agonist 10

Copy Product Info
🥰Excellent
Catalog No. T213214

THR-β agonist 10 is an orally active and selective THR-β agonist with an EC50 value of 11 nM. It effectively lowers levels of ALT (alanine aminotransferase), TC (total cholesterol), and LDL-C (low-density lipoprotein cholesterol). In mouse models of metabolic dysfunction-associated steatohepatitis (MASH), it improves steatosis, ballooning, inflammation, and fibrosis. THR-β agonist 10 is utilized in the research of MASH.

THR-β agonist 10
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction

Bioactivity
Description
THR-β agonist 10 is an orally active and selective THR-β agonist with an EC50 value of 11 nM. It effectively lowers levels of ALT (alanine aminotransferase), TC (total cholesterol), and LDL-C (low-density lipoprotein cholesterol). In mouse models of metabolic dysfunction-associated steatohepatitis (MASH), it improves steatosis, ballooning, inflammation, and fibrosis. THR-β agonist 10 is utilized in the research of MASH.
Targets&IC50
THRβ:11 nM (EC50)
In vitro
THR-β agonist 10 (Compound 12) exhibits strong agonistic activity on THR-β, with an EC₅₀ of 11.0 nM. It shows no significant cytotoxicity in primary mouse and rat hepatocytes at concentrations ranging from 0 to 100 μM over 24 hours. The compound demonstrates weak inhibition of CYP2C9 with an IC₅₀ of 9.4 μM, but does not inhibit other CYP enzymes (CYP1A2, 2C19, 2D6, 3A4-M, 3A4-T) at concentrations where IC₅₀ exceeds 25 μM.
In vivo
THR-β agonist 10 (Compound 12) administered orally at 3 mg/kg significantly reduces serum total cholesterol and low-density lipoprotein cholesterol in mice. Moreover, a daily oral dose of THR-β agonist 10 at 1-3 mg/kg for six weeks markedly decreases serum alanine aminotransferase, total cholesterol, and low-density lipoprotein cholesterol levels in mice with metabolic associated steatohepatitis (MASH).
Chemical Properties
Storage & Solubility Information
StoragePowder: -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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
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