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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.

For research use only. We do not sell to patients.

Formula: C₂₅H₂₀O₃
Molecular Weight:368.42

Storage:

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

Data Sheet (275 KB)

PPARα agonist 5 Chemical Structure

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

PPARα

3 nM (EC₅₀)

PPAR-γ

1.66 μM (EC₅₀)

PPARδ

>25 μM (EC₅₀)

All PPAR Isoforms :

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.

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	T_1/2	V_d	Clearance (CL)	MRT	T_max	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.

Chemical Information

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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Laghezza A, et al. A new potent and selective peroxisome proliferator-activated receptor alpha partial agonist displays anti-steatotic effects In vitro and behaves as a safe hypolipidemic and hypoglycemic agent in a diabetic mouse model. Eur J Med Chem. 2025 May 5;289:117494. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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