THR-β agonist 12
THR-β agonist 12 is an orally active, potent, and highly selective thyroid hormone receptor β (THR-β) agonist (EC50 = 36 nM). THR-β agonist 12 shows no significant activity against THRα and exhibits no cardiotoxicity in vivo. THR-β agonist 12 inhibits lipid synthesis by activating the AMPK-ACC-SREBP1 signaling axis. THR-β agonist 12 can be used on research into metabolic dysfunction-associated steatohepatitis (MASH) and related metabolic diseases.
For research use only. We do not sell to patients.
- CAS No.: 3063509-17-8
- Formula: C17H9Cl3F3NO3
- Molecular Weight:438.61
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Biological Activity
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AMPK |
THR-β agonist 12 (compound 14q) (0.001-100 μM; 24 h) shows no significant cytotoxicity and dose not affect cell proliferation in A2780, Hepa1-6, and HepG2 cells[1].
THR-β agonist 12 (1-100 μM; 24 h) significantly inhibits lipid accumulation in FFA (free fatty acid)-induced HepG2 cells[1].
THR-β agonist 12 (1-100 μM; 24 h) reduces intracellular triglyceride (TG) and total cholesterol (TC) levels in FFA-induced HepG2 cells. THR-β agonist 12 reduces the release of aspartate aminotransferase (AST) and alanine aminotransferase (ALT) into the culture medium in a concentration-dependent manner, thereby alleviating cellular injury in FFA-induced HepG2 cells. THR-β agonist 12 inhibits reactive oxygen species (ROS) production in a concentration-dependent manner, exerting an antioxidant effect in FFA-induced HepG2 cells. THR-β agonist 12 activates the AMPK-ACC-SREBP1 signaling pathway in FFA-induced HepG2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A2780 cells, Hepa1-6 cells, HepG2 cells
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Concentration:0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 10μM, 100 μM
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Incubation Time:24 h
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Result:Did not affect cell viability and exhibited a good safety profile.
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Cell Line:HepG2 cells (FFA-induced)
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Concentration:1 μM, 10 μM, 100 μM
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Incubation Time:24 h
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Result:Increased the ratios of p-AMPK/AMPK and p-ACC/ACC, and simultaneously decreased the protein expression level of SREBP1.
| Species | Dose | Route | AUC0-∞ | Tmax | Cmax | T1/2 | F | CL | Vd |
|---|---|---|---|---|---|---|---|---|---|
| Mice | 10 mg/kg | p.o. | 15.24 h·μg/L | 0.500 h | 5.69 μg/mL | 1.95 h | 102.45 % | / | / |
| Mice | 2 mg/kg | i.v. | 2.99 μg·h/mL | 0.0830 h | 4.21 μg/mL | 1.23 h | / | 11.51 mL/min/kg | 0.670 L/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (male, 5-6 weeks old, 18-20 g) were fed a methionine-choline-deficient (MCD) diet for 4 consecutive weeks to establish the MASH mouse model[1].
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Dosage:3 mg/kg or 10 mg/kg
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Administration:o.p., once daily, for 30 days
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Result:Decreased the quantity and size of lipid droplets in the liver in a dose-dependent manner, significantly ameliorating hepatic steatosis.
Significantly reduced the elevated serum triglyceride (TG) and total cholesterol (TC) levels.
Significantly decreased plasma aspartate aminotransferase (AST) and alanine aminotransferase (ALT) levels, alleviating hepatocellular injury.
Significantly upregulated the mRNA expression levels of THR-β target genes (Thrsp, Dio1, and Me1) in the liver, activating the hepatic THR-β signaling pathway.
Did not alter the mRNA expression levels of Myh6 or Myh7, nor the Myh6/Myh7 ratio in the heart, indicating that it did not induce cardiotoxicity.
Chemical Information
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CAS No. 3063509-17-8
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Molecular Weight 438.61
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Formula C17H9Cl3F3NO3
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SMILES
ClC1=C2C(NC(C(O)=O)=C2)=CC(Cl)=C1OCC3=C(C(C(F)(F)F)=CC=C3)Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
THR-β agonist 12 Related Classifications
HY-184939 Related Classifications
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