2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR Phosphatase
  4. PPARα agonist 5

PPARα agonist 5 is an orally available, selective partial agonist of PPARα (EC50: 3 nM). PPARα agonist 5 reduces lipid accumulation and upregulates key PPARα target genes, exerting anti-fatty liver effects. PPARα agonist 5 also exhibits significant hypolipidemic and hypoglycemic effects through partial PPARγ agonist activity and mild inhibition of protein tyrosine phosphatase 1B (PTP1B) (IC50: 79.1 μM). PPARα agonist 5 has a good safety profile and can be used in the study of type 2 diabetes with dyslipidemia.

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PPARα agonist 5

PPARα agonist 5 Chemical Structure

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PPARα agonist 5 Related Antibodies

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Description

PPARα agonist 5 is an orally available, selective partial agonist of PPARα (EC50: 3 nM). PPARα agonist 5 reduces lipid accumulation and upregulates key PPARα target genes, exerting anti-fatty liver effects. PPARα agonist 5 also exhibits significant hypolipidemic and hypoglycemic effects through partial PPARγ agonist activity and mild inhibition of protein tyrosine phosphatase 1B (PTP1B) (IC50: 79.1 μM). PPARα agonist 5 has a good safety profile and can be used in the study of type 2 diabetes with dyslipidemia[1].

IC50 & Target

PPARα

3 nM (EC50)

PPAR-γ

1.66 μM (EC50)

PPARδ

>25 μM (EC50)

In Vitro

PPARα agonist 5 (Compound (S)-2) selectively agonizes PPARα in HepG2 cells (EC50: 3 nM), is approximately 550-fold more active against PPARα than against PPARγ (EC50: 1.66 μM), and has no significant activity against PPARδ[1].
PPARα agonist 5 (0.025-25 μM, 24 h/15days) significantly reduces lipid accumulation induced by oleic acid in HepaRG cells and upregulated PPARα target genes associated with fatty acid oxidation, indicating that it exerts anti-fatty liver effects by activating lipid metabolism pathways[1].

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

PPARα agonist 5 Related Antibodies

Real Time qPCR[1]

Cell Line: oleic acid (500 μM) treated HepaRG cells
Concentration: 0.025, 0.25, 2.5, 25 μM
Incubation Time: oleic acid for 24 hours, then for another 24 hours or 15 days
Result: Significantly upregulated fatty acid oxidation-related genes (CPT1a, HMGCS2, PDK4), and the activation of these genes indicated that it promoted fatty acid oxidation and reduced liver fat accumulation.
Parmacokinetics
Species Dose Route Plasma Concentration AUC T1/2 Vd Clearance (CL) MRT Tmax Bioavailability
Mice[1] 1 mg/kg i.v. 11700 ng/mL 8160 ng·h/mL 3.21 h 0.536 L/kg 1.99 mL/min/kg 2.32 h / /
Mice[1] 5 mg/kg p.o. 5880 ng/mL 35700 ng·h/mL 5.63 h 1.12 L/kg 2.27 mL/min/kg 5.58 h 1 h 87.6 %
In Vivo

PPARα agonist 5 (Compound (S)-2) (1-7.5 mg/kg, p.o. 7 consecutive days) shows significant lipid-lowering and blood sugar-lowering effects in the Tyloxapol (HY-B1068)-induced hyperlipidemia diabetic mouse model, and is non-toxic to arteries, kidneys, liver and pancreas, and can improve tissue damage caused by hyperlipidemia[1].

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

Animal Model: Swiss Albino mice (male, weight 25-30 g) injected with Tyloxapol (400 mg/kg)[1]
Dosage: (1, 3, 7.5 mg/kg)
Administration: p.o. 7 consecutive days
Result: Significantly reduced total cholesterol (TC), triglycerides (TG), low-density lipoprotein (LDL-C) and very low-density lipoprotein (VLDL-C) levels.
Showed significant hypoglycemic effects, which were associated with its partial PPARγ agonist activity and mild inhibition of protein tyrosine phosphatase 1B (PTP1B).
Was non-toxic to arteries, kidneys, liver and pancreas at a dose of 3 mg/kg, and was able to reverse organ damage caused by hyperlipidemia.
Molecular Weight

368.42

Formula

C25H20O3
SMILES

O=C(O)[C@@](C1=CC=CC=C1)(C)OC(C=C2)=CC=C2C3=C(C=CC=C4)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 agonist 5 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 agonist 5PPARα agonist5PPARα agonist-5PPARPhosphatasePeroxisome proliferator-activated receptorshypolipidemic and hypoglycemic activityHepaRG cellsHyperlipidemic micePTP1BInhibitorinhibitorinhibit

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