1. Vitamin D Related/Nuclear Receptor
  2. Thyroid Hormone Receptor
  3. THR-β agonist 11

THR-β agonist 11 is an orally active and selective thyroid hormone receptor (THR-β) agonist. THR-β agonist 11 shows potent cholesterol-lowering activity in cholesterol-fed rats. THR-β agonist 11 significantly reduces serum total TG, LDL-cholesterol, liver total TC and TG levels, and alleviates hepatic steatosis, inflammation and fibrosis in HFD-CCl4-induced Metabolic dysfunction-associated steatohepatitis (MASH) model mice. THR-β agonist 11 can be used for the study of metabolic dysfunction-associated steatohepatitis (MASH) and other fibrotic diseases.

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THR-β agonist 11

THR-β agonist 11 Chemical Structure

CAS No. : 3051970-23-8

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Description

THR-β agonist 11 is an orally active and selective thyroid hormone receptor (THR-β) agonist. THR-β agonist 11 shows potent cholesterol-lowering activity in cholesterol-fed rats. THR-β agonist 11 significantly reduces serum total TG, LDL-cholesterol, liver total TC and TG levels, and alleviates hepatic steatosis, inflammation and fibrosis in HFD-CCl4-induced Metabolic dysfunction-associated steatohepatitis (MASH) model mice. THR-β agonist 11 can be used for the study of metabolic dysfunction-associated steatohepatitis (MASH) and other fibrotic diseases[1].

In Vivo

THR-β agonist 11 (Compound 29a) (0.5 mg/kg, p.o., single administration, 24 h) exhibits a superior cholesterol-lower effect in cholesterol-fed Sprague-Dawley rats[1].
THR-β agonist 11 (3 mg/kg, p.o., once daily, 6 weeks) significantly reduces serum total TG, LDL-cholesterol, liver total TC and TG levels in HFD-CCl4-induced MASH model C57BL/6J mice[1].

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

Animal Model: Male Sprague-Dawley rats were fed a normal chow diet supplemented with 1.5% cholesterol and 0.5% cholic acid (w/w) for 2 weeks to establish the model[1]
Dosage: 0.5 mg/kg
Administration: p.o., single administration, 24 h
Result: Achieved a total plasma cholesterol reduction rate of 29.07%.
Animal Model: 4-week-old male C57BL/6J mice were fed a high-fat diet (HFD) for 10 weeks to induce obesity, then intraperitoneally injected with carbon tetrachloride (CCl4) twice a week for 6 weeks to establish the MASH model[1]
Dosage: 3 mg/kg
Administration: p.o., once daily, 6 weeks
Result: Reduced serum total TG, LDL-cholesterol, liver total TC and TG levels.
Decreased serum ALT and AST levels by a notable margin.
Alleviated hepatic steatosis, inflammation and fibrosis.
Downregulated the mRNA expression levels of fibrosis markers Tgfb1 and Acta2.
Molecular Weight

516.95

Formula

C26H30ClN2O5P

CAS No.
SMILES

CC1=CC(OC[P@]2(OCC[C@H](O2)C3=CC=CC(Cl)=C3)=O)=CC(C)=C1CC4=NNC(C(C(C)C)=C4)=O

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Product Name:
THR-β agonist 11
Cat. No.:
HY-178015
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