1. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation NF-κB
  2. PPAR Glutathione Peroxidase SOD TNF Receptor Interleukin Related NF-κB
  3. 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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PPARγ agonist 20

PPARγ agonist 20 Chemical Structure

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Description

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[1].

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

PPARγ agonist 20 (50 mg/kg, p.o., once daily for 28 days) exhibits significant antidiabetic activity in a Streptozotocin (STZ)-nicotinamide-induced diabetic rat model[1].

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

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].
Dosage: 50 mg/kg
Administration: P.o., once daily for 28 days
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.
Molecular Weight

537.97

Formula

C25H20ClN5O5S

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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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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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.

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Product Name:
PPARγ agonist 20
Cat. No.:
HY-178447
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