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^[1].

IC50: 0.03 μM (THR-β) and 0.22 μM (THR-α)^[1]

THR-β agonist 6 (3, 10 mg/kg; Orally; once daily for 6 weeks) prominently reduces HFD-CCl4-induced (CCl4; ip; 0.05 mL/kg) serum total cholesterol and LDL-cholesterol levels in a dose-dependent manner^[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

457.27

C₂₀H₁₄Cl₂N₆O₃

2791290-58-7

CC(C)N1C(C=CC2=C1C=CN2C3=C(Cl)C=C(N4N=C(C#N)C(NC4=O)=O)C=C3Cl)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Liuyu Hu, et al. Discovery of Highly Potent and Selective Thyroid Hormone Receptor β Agonists for the Treatment of Nonalcoholic Steatohepatitis. J Med Chem. 2023 Mar 9;66(5):3284-3300.  [Content Brief]