ZG-2585
ZG-2585 is an orally active and selective thyroid hormone receptor β (THRβ) agonist. ZG-2585 selectively activates THRβ over THRα, driving allosteric conformational changes and coactivator recruitment. ZG-2585 reduces body weight, hepatic steatosis and lipid accumulation in a Western diet-induced metabolic disorder model. ZG-2585 can be used for the research of metabolic disorders, including obesity, dyslipidemia and metabolic dysfunction-associated steatohepatitis.
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- CAS No.: 3052796-86-5
- Formule: C19H17Cl2N3O4
- Masse moléculaire:422.26
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
ZG-2585 (compound 18) stably binds within the THRβ ligand-binding pocket, forming critical salt bridge and hydrogen bond interactions with key residues including Arg320, Arg316, Arg282, Asn331, and His435 over 100 ns of molecular dynamics simulation[1].
ZG-2585 shows suitable metabolic stability in rat liver microsomes, with a T1/2 of 204 min and CLint of 3.4 μL/min/mg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
ZG-2585 (5-20 mg/kg; p.o.; every other day; 30 days) dose-dependently reduces body weight, hepatic steatosis, and lipid accumulation in western-diet-induced metabolic disorder mice, with 20 mg/kg inducing an 11.73% body weight reduction and normalizing liver weights[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 6 weeks old, western-diet-induced metabolic disorder)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:p.o.; every other day; 30 days
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Result:Reduced body weight, liver weight and inguinal white adipose tissue mass dose-dependently at 5/10/20 mg/kg vs vehicle baseline.
Lowered serum total cholesterol, LDL-C, hepatic total cholesterol and triglyceride in a dose-dependent manner, while serum triglyceride stayed unaltered.
Diminished serum AST and ALT levels with rising dosage across all treatment groups.
Suppressed hepatic lipid droplet accumulation and shrank i-WAT adipocytes, with maximal efficacy at 20 mg/kg.
Elevated hepatic mRNA expression of THR target genes markedly at 10 mg/kg.
Produced no meaningful alterations in cardiac Myh6, Myh7, Klf9, Hr transcripts or the Myh6/Myh7 expression ratio.
Chemical Information
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CAS No. 3052796-86-5
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Masse moléculaire 422.26
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Formule C19H17Cl2N3O4
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SMILES
CC(N1C(C=CC2=C1C=CN2C3=C(C=C(C=C3Cl)C(NCC(O)=O)=O)Cl)=O)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ZG-2585 Related Classifications
HY-187505 Related Classifications
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