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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.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| 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). |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
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
and mix thoroughly until a homogeneous solution is obtained.
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