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.
For research use only. We do not sell to patients.
- Formula: C25H13Cl2N7O3
- Molecular Weight:530.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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THR-β 11 nM (EC50) |
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 (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.
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Animal Model:7-8 week-old male ICR mice[1]
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Dosage:3 mg/kg
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Administration:p.o., single dose
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Result:Reduced serum total cholesterol by 34.2% and low-density lipoprotein cholesterol by 56.3%.
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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]
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Dosage:1 mg/kg or 3 mg/kg
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Administration:p.o., once daily, 6 weeks
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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.
Chemical Information
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Molecular Weight 530.32
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Formula C25H13Cl2N7O3
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
THR-β agonist 10 Related Classifications
HY-175676 Related Classifications
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