2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR
  4. PPARα/γ agonist 4

PPARα/γ agonist 4 (Compound (S)-7) is an orally active dual potent agonist of PPARα and PPARγ, with EC50 values of 0.061 μM and 1.42 μM respectively. PPARα/γ agonist 4 acts through an insulin-independent mechanism and exhibits mitochondrial pyruvate carrier inhibition and anti-diabetic properties. PPARα/γ agonist 4 is expected to be used in research for dyslipidemic type 2 diabetes.

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PPARα/γ agonist 4 Chemical Structure

PPARα/γ agonist 4 Chemical Structure

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PPARα/γ agonist 4 Related Antibodies

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Description

PPARα/γ agonist 4 (Compound (S)-7) is an orally active dual potent agonist of PPARα and PPARγ, with EC50 values of 0.061 μM and 1.42 μM respectively. PPARα/γ agonist 4 acts through an insulin-independent mechanism and exhibits mitochondrial pyruvate carrier inhibition and anti-diabetic properties. PPARα/γ agonist 4 is expected to be used in research for dyslipidemic type 2 diabetes[1].

IC50 & Target[1]

PPARα

 

PPAR-γ

 

In Vitro

PPARα/γ agonist 4 (100 nM, 24 h) is able to increase the uptake and metabolism of glucose in C2C12 cell line and enhance mitochondrial activity by boosting fatty acid degradation, thus avoiding lipid accumulation in liver or muscle cells [1].

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

PPARα/γ agonist 4 Related Antibodies
In Vivo

PPARα/γ agonist 4 (25 mg/kg, 50 mg/kg, p.o., a period of 15 days) exhibits dose-dependent antihyperglycemic effects in diabetic mouse models, along with lipid-lowering efficacy[1].

Pharmacokinetic Analysis in MC38 Syngeneic Model[1]

PPARα/γ agonist 4 Does Volume (mL/kg) C0/Cmax(ng/mL) Tmax (h) AUClast(h·ng/mL) AUCinfinity (h⋅ng/mL) T1/2 (h) Vd (L/kg) CL (mL/min/kg) MRTlast(h) F (%)
i.v. (1 mg/kg) 10 2300 0.083 11400 11800 4.74 0.581 1.42 6.04 -
p.o. (5 mg/kg) 10 4280 2 43600 49000 7.61 1.16 1.74 7.74 76.4

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

Animal Model: Streptozotocin (HY-13753) -induced diabetic mouse model[1]
Dosage: 25 mg/kg, 50 mg/kg
Administration: Oral gavage (p.o.), 15 days
Result: At a dose of 50 mg/kg exhibited greater hypoglycemic effects compared to the 25 mg/kg dose.
Oral treatment with PPARα/γ agonist 4 at 25 mg/kg significantly reduced levels of total cholesterol, high-density lipoprotein cholesterol (HDL-C), low-density lipoprotein cholesterol (LDL-C), and triglycerides.
The 50 mg/kg dose reduced total cholesterol and HDL-C levels, but showed a smaller improvement in triglyceride levels.
Molecular Weight

368.42

Formula

C25H20O3
SMILES

O=C(O)[C@H](CC1=CC=CC=C1)OC2=CC=C(C=C2)C3=C4C(C=CC=C4)=CC=C3
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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PPARα/γ agonist 4 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:

PPARα/γ agonist 4PPARPeroxisome proliferator-activated receptorsC2C12 cell lineDiabetic mouse modelMitochondrial pyruvate carrier inhibitionAntidiabetic propertiesDiabetesInhibitorinhibitorinhibit

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