THR-β agonist 9
THR-β agonist 9 is a potent, selective, and His435 mutation-sensitive THR-β (EC50: 3.2 nM) agonist. THR-β agonist 9 has moderate selectivity (approximately 10-fold) and good activation capacity (EC50: 134.2 nM to 515.5 nM) for multiple His435 mutants (H435A, H435Y, and H435R). THR-β agonist 9 has the potential to be used in the study of dyslipidemia, metabolic dysfunction-associated steatohepatitis (MASH), or resistance to thyroid hormone (RTH).
For research use only. We do not sell to patients.
- CAS No.: 2920045-74-3
- Formula: C23H18N2O6
- Molecular Weight:418.40
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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
THR-β with an EC50 of 258.2 nM[1]
THR-β agonist 9 (Compound 15n) (1 μM) can activate THR-β with an EC50 of 258.2 nM and a potency of 1707.0 nM for THR-α, showing excellent selectivity in cell-based reporter gene assays[1].
THR-β agonist 9 simultaneously activates three mutants with EC50s of THR-βH435A (515.5 nM), THR-βH435R (134.2 nM) and THR-βH435Y (513.1 nM)[1].
THR-β agonist 9 (1-10 μM, 24 hours) can reduce TG and TC levels and lipid accumulation in mouse primary hepatocytes and HepG2 cells[1].
THR-β agonist 9 (1-10 μM, 24 hours) increases basal and uncoupled mitochondrial respiration in HepG2 cells[1].
THR-β agonist 9 (1-10 μM, 24 hours) increases the phosphorylation of AMPK and ACC, accompanied by higher CPT1 protein levels, improving the metabolism of HepG2 cells through the AMPK pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:1 μM, 3 μM, 10 μM
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Incubation Time:
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Result:Increased phosphorylation of AMPK and ACC, accompanied by higher protein levels of CPT1.
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Cell Line:THR-β-positive cells (HepG2 and primary mouse liver cells) and a THRβ-negative cell lines (NCIH460, lung cancer)
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Concentration:10 μM
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Incubation Time:72 h
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Result:Did not show cell proliferation inhibition activity in two THR-β-positive HepG2 cells and NCIH460.
| Species | Dose | Route | AUC0-∞ | Tmax | Cmax | T1/2 | F | Vz | Clmax |
|---|---|---|---|---|---|---|---|---|---|
| Rat | 10 mg/kg | p.o. | 8.57 μg·h/mL | 0.50 h | 3.79 μg/mL | 2.37 h | 86.10 % | / | / |
| Rat | 5 mg/kg | i.v. | 4.98 μg·h/mL | 0.08 h | 7.10 μg/mL | 1.30 h | / | 1.90 L/kg | 1.01 mL/min/kg |
Chemical Information
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CAS No. 2920045-74-3
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Molecular Weight 418.40
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Formula C23H18N2O6
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SMILES
OC1=C(C(NCC(O)=O)=O)N=C(OC)C2=CC(OC3=CC=C4C(C=CC=C4)=C3)=CC=C21
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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 9 Related Classifications
HY-174887 Related Classifications
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