2. Vitamin D Related/Nuclear Receptor
  3. Thyroid Hormone Receptor
  4. THR-β agonist 10

THR-β agonist 10 is an orally active and selective THR-β agonist, with an EC50 of 11 nM. THR-β agonist 10 significantly reduces ALT (Alanine Aminotransferase), TC (Total Cholesterol), and LDL-C (Low-Density Lipoprotein Cholesterol) levels, and improves steatosis, ballooning, inflammation and fibrosis in the metabolic dysfunction-associated steatohepatitis (MASH) mouse model. THR-β agonist 10 can be used for the study of MASH.

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THR-β agonist 10

THR-β agonist 10 Chemical Structure

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THR-β agonist 10 Related Antibodies

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Description

THR-β agonist 10 is an orally active and selective THR-β agonist, with an EC50 of 11 nM. THR-β agonist 10 significantly reduces ALT (Alanine Aminotransferase), TC (Total Cholesterol), and LDL-C (Low-Density Lipoprotein Cholesterol) levels, and improves steatosis, ballooning, inflammation and fibrosis in the metabolic dysfunction-associated steatohepatitis (MASH) mouse model. THR-β agonist 10 can be used for the study of MASH[1].

IC50 & Target[1]

THR-β

11 nM (EC50)

In Vitro

THR-β agonist 10 (Compound 12) (16 h) exhibits potent agonistic activity against THR-β with an of EC50 11.0 nM[1].
THR-β agonist 10 (0-100 μM, 24 h) shows no obvious cytotoxicity in primary mouse hepatocytes and primary rat hepatocytes[1].
THR-β agonist 10 (exerts weak inhibition on CYP2C9 (IC50 = 9.4 μM) but no inhibitory effect on other CYP enzymes (CYP1A2, 2C19, 2D6, 3A4-M, 3A4-T) with IC50 > 25 μM[1].

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

THR-β agonist 10 Related Antibodies
In Vivo

THR-β agonist 10 (Compound 12) (3 mg/kg, p.o., single dose) significantly reduces serum total cholesterol and low-density lipoprotein cholesterol in mice[1].
THR-β agonist 10 (1-3 mg/kg, p.o., once daily, 6 weeks) significantly decreases serum alanine aminotransferase, total cholesterol and low-density lipoprotein cholesterol levels in mice with metabolic-disorder-associated steatohepatitis (MASH)[1].

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

Animal Model: 7-8 week-old male ICR mice[1]
Dosage: 3 mg/kg
Administration: p.o., single dose
Result: Reduced serum total cholesterol by 34.2% and low-density lipoprotein cholesterol by 56.3%.
Animal Model: Male C57BL/6J mice (for MASH model): 4-5 week-old male C57BL/6J mice were first fed a high-fat diet for 14 weeks to induce obesity, then received intraperitoneal injections of Carbon tetrachloride (HY-Y0298) twice a week for an additional 6 weeks to establish the MASH model[1]
Dosage: 1 mg/kg or 3 mg/kg
Administration: p.o., once daily, 6 weeks
Result: Achieved significant decreases in serum alanine aminotransferase, total cholesterol, and low-density lipoprotein cholesterol levels.
Achieved reductions in NAFLD Activity Score (NAS) by improving steatosis, ballooning, and inflammation.
Showed effective alleviation of liver fibrosis.
Molecular Weight

530.32

Formula

C25H13Cl2N7O3
SMILES

O=C1NC(N(C2=CC(Cl)=C(N3C=CC4=C3C=CC(N4CC5=CC=C(C#N)C=C5)=O)C(Cl)=C2)N=C1C#N)=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 10 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

THR-β agonist 10Thyroid Hormone ReceptorTHRmetabolic dysfunction-associated steatohepatitisALT (Alanine Aminotransferase)TC (Total Cholesterol)LDL-C (Low-Density Lipoprotein Cholesterol)THR-βInhibitorinhibitorinhibit

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