THR-β agonist 6
THR-β agonist 6 is an orally active, selective thyroid hormone receptor β (THR-β) agonist with EC50s of 0.03 μM and 0.22 μM for THR-β and THR-α, respectively. THR-β agonist 6 exhibits an xcellent liver-to-serum ratio of 93:1 in mice. THR-β agonist 6 has the potential for nonalcoholic steatohepatitis (NASH) research.
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- CAS No.: 2791290-58-7
- Formule: C20H14Cl2N6O3
- Masse moléculaire:457.27
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Stockage:
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Activité biologique
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Chemical Information
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Activité biologique
IC50: 0.03 μM (THR-β) and 0.22 μM (THR-α)[1]
THR-β agonist 6 (3, 10 mg/kg; po; single dose) displays over 30% reduction of TC and potently decreases serum LDL-C (LDL-cholesterol) levels by 62.1 and 53.6% at both 10 and 3 mg/kg with efficacy in ICR mice[1].
THR-β agonist 6 (3, 10 mg/kg; po; single dose) significantly upregulates the Dio1, Thrsp, and Me1 mRNA levels by above 19-, 16-, and 3-fold[1].
Pharmacokinetic Parameters of THR-β agonist 6 in mice[1].
| PO (30 mg/kg) | |
| Tmax (h) | 8.7 |
| Cmax (ng/mL) | 2830 |
| AUClast (h*ng/mL) | 37536 |
| t1/2 (h) | 8.7 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice (4-5 weeks) fed a high-fat diet (HFD) for 10 weeks[1]
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Dosage:3, 10 mg/kg
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Administration:Orally; once daily for 6 weeks
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Result:Prominently reduced HFD-CCl4-induced (CCl4; ip; 0.05 mL/kg) serum total cholesterol and LDL-cholesterol levels in a dose-dependent manner.
Markedly reduced the liver steatosis and inflammation score.
Chemical Information
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CAS No. 2791290-58-7
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Masse moléculaire 457.27
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Formule C20H14Cl2N6O3
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SMILES
CC(C)N1C(C=CC2=C1C=CN2C3=C(Cl)C=C(N4N=C(C#N)C(NC4=O)=O)C=C3Cl)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
THR-β agonist 6 Related Classifications
HY-149218 Related Classifications
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