PPARγ agonist 20
PPARγ agonist 20 is a potent, orally active PPAR-γ agonist. PPARγ agonist 20 effectively increases antioxidant defenses (SOD, GSH) and reduces lipid peroxidation. PPARγ agonist 20 can upregulate of Pparg, Glut4, and AdipoQ, suppresses of TNF-α, IL-6, and NF-κB p65. PPARγ agonist 20 significantly lowers fasting blood glucose, improving glucose tolerance, and restoring metabolic balance in Streptozotocin (HY-13753)-Nicotinamide (HY-B0150)-induced diabetic rats. PPARγ agonist 20 can be used for the study of type 2 diabetes.
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- Formule: C25H20ClN5O5S
- Masse moléculaire:537.97
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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
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Activité biologique
Description
In Vitro
PPARγ agonist 20 (Compound 7e) (6.25-100 μM) induces a significantly high expression of PPAR-γ in HepG2 cells and L6 myotubes[1].
PPARγ agonist 20 exhibits good inhibitory activity against α-amylase (IC50 = 23.3 μg/mL) and α-glucosidase (IC50 = 21.1 μg/mL)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-inf | AUC0-t |
|---|---|---|---|---|---|---|---|
| Rat | 50 mg/kg | p.o. | 4 h | 3 h | 2.069 μg/mL | 13.04 μg·h/mL | 11.87 μg·h/mL |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A single intraperitoneal dose of STZ (45 mg/kg body weight), administered 20 min after intraperitoneal injection of nicotinamide (110 mg/kg body weight), resulted in the induction of type 2 diabetes mellitus in the male Wistar rats (160.23 ± 10.00 g)[1].
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Dosage:50 mg/kg
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Administration:P.o., once daily for 28 days
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Result:Led to a significant and dose-dependent improvement in body weight, and mitigated diabetes-associated muscle wasting and metabolic decline.
Effectively controlled hyperglycemia by enhancing insulin sensitivity and glucose handling.
Significantly reduced serum alanine aminotransferase (SGPT), serum aspartate aminotransferase (SGOT), and alkaline phosphatase (ALP) levels.
Significantly reduced the levels of urea, creatinine, and uric acid.
Significantly improved lipid profile: reduced TG, TC, LDL, and VLDL, and increased HDL.
Upregulated metabolic genes (Pparg, Glut4, AdipoQ) and downregulated inflammatory genes (TNF-α, IL-6).
Increased PPAR-γ protein expression and inhibited NF-κB p65.
Reversed tissue damage caused by diabetes, including adipose tissue, pancreas, liver, and skeletal muscle.
Chemical Information
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Masse moléculaire 537.97
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Formule C25H20ClN5O5S
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SMILES
COC1=CC(/C=N/NC(N/N=C/C2=CC=C(C(O)=C2O)O)=S)=CC=C1OC3=CC=NC4=CC(Cl)=CC=C43
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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)
PPARγ agonist 20 Related Classifications
HY-178447 Related Classifications
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