PPARα agonist 5

Cat. No.: HY-173217: FAQs
Data Sheet Handling Instructions Technical Support

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.

PPARα agonist 5 Chemical Structure

Size		Stock
MOQ		Minimum order quantity
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All PPAR Isoform Specific Products:

View All Isoforms

PPARα PPARβ/δ PPARγ PPAR PPARδ

Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

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^[1]

Species	Dose	Route	Indicator	value
Mice	1 mg/kg	i.v.	C_min	11700 ng/mL
Mice	5 mg/kg	p.o.	C_max	5880 ng/mL
Mice	1 mg/kg	i.v.	AUC_0-t	8160 ng·h/mL
Mice	5 mg/kg	p.o.	T_max	1 hr
Mice	1 mg/kg	i.v.	AUC_0-inf	8620 ng·h/mL
Mice	5 mg/kg	p.o.	AUC_0-t	35700 ng·h/mL
Mice	1 mg/kg	i.v.	T_1/2	3.21 hr
Mice	5 mg/kg	p.o.	AUC_0-inf	37200 ng·h/mL
Mice	1 mg/kg	i.v.	V_d	0.536 L/kg
Mice	5 mg/kg	p.o.	T_1/2	5.63 hr
Mice	1 mg/kg	i.v.	CL	1.99 mL/min/kg
Mice	5 mg/kg	p.o.	V_d	1.12 L/kg
Mice	1 mg/kg	i.v.	MRT_0-t	2.32 hr
Mice	5 mg/kg	p.o.	CL	2.27 mL/min/kg
Mice	5 mg/kg	p.o.	MRT_0-t	5.58 hr
Mice	5 mg/kg	p.o.	F	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

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]

PPARα agonist 5 Related Classifications

Metabolic Disease Cardiovascular Disease

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *