1. Vitamin D Related/Nuclear Receptor
  2. Thyroid Hormone Receptor
  3. 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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THR-β agonist 6 Chemical Structure

THR-β agonist 6 Chemical Structure

CAS No. : 2791290-58-7

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Description

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 & Target

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

In Vivo

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].

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.

Animal Model: Male C57BL/6J mice (4-5 weeks) fed a high-fat diet (HFD) for 10 weeks[1]
Dosage: 3, 10 mg/kg
Administration: Orally; once daily for 6 weeks
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.
Molecular Weight

457.27

Formula

C20H14Cl2N6O3

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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THR-β agonist 6 Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
THR-β agonist 6
Cat. No.:
HY-149218
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