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Cat. No.: HY-183318

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PPARα/δ agonist 4

PPARα/δ agonist 4 is a potent orally active and selective dual peroxisome proliferator-activated receptor (PPAR) α/δ agonist with EC₅₀s of 0.36 and 1.31 nM, respectively. PPARα/δ agonist 4 exhibits >123-fold selectivity over PPARγ (EC₅₀ = 160.84 nM). PPARα/δ agonist 4 upregulates expression of downstream fatty acid oxidation genes PDK4, CPT1A, and ACADVL. PPARα/δ agonist 4 can be used for the research of metabolic dysfunction-associated steatohepatitis.

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

CAS No.: 3108258-69-8
Formula: C₂₂H₂₄N₄O₆
Molecular Weight:440.45

Storage:

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

PPARα/δ agonist 4 Chemical Structure

CAS No.: 3108258-69-8

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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
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

PPARα

0.36 nM (EC₅₀)

PPARδ

1.31 nM (EC₅₀)

PPARγ

160.84 nM (EC₅₀)

All PPAR Isoforms :

In Vitro

PPARα/δ agonist 4 (compound A32) (20 nM) acts as a potent agonist of hPPARδ, achieving 94% activation at 20 nM in a Gal4-based transactivation assay^[1].
PPARα/δ agonist 4 exhibits high metabolic stability in human, rat, and mouse liver microsomes^[1].
PPARα/δ agonist 4 does not significantly inhibit major human CYP isoforms (CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4)^[1].
PPARα/δ agonist 4 (30 μM) shows minimal hERG channel inhibition (7.80%), indicating a favorable cardiac safety profile^[1].
PPARα/δ agonist 4 (8-200 nM; 12 h) upregulates the expression of PPARα/δ downstream fatty acid oxidation genes (PDK4, CPT1A, ACADVL) in HepG2 cells^[1].
PPARα/δ agonist 4 forms stable, high-affinity interactions with hPPARα and hPPARδ via specific hydrogen bonds, while exhibiting weaker binding to hPPARγ, consistent with its in vitro selectivity profile^[1].

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

Real Time qPCR^[1]

Cell Line:

HepG2
Concentration:

8; 200 nM
Incubation Time:

12 h
Result:

Increased the expression of PDK4, CPT1A, and ACADVL in HepG2 cells.
Induced a markedly stronger upregulation of PDK4 and a slightly greater induction of CPT1A and ACADVL relative to Elafibranor (HY-16737).

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t
Rat^[1]	10 mg/kg	i.g.	6.47 h	0.38 h	10770 ng/mL	22450 ng·h/mL
Dog^[1]	5 mg/kg	i.g.	13.60 h	0.50 h	33500 ng/mL	203000 ng·h/mL

In Vivo

PPARα/δ agonist 4 (compound A32) (10 mg/kg; p.o.; single dose) exhibits pronounced liver targeting in male SD rats, with liver concentrations substantially higher than those in other tissues and minimal distribution to the brain and CSF^[1].

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

Animal Model:

Sprague-Dawley (male, 204-239 g)^[1]
Dosage:

10 mg/kg
Administration:

p.o.; single dose
Result:

Was predominantly distributed to the liver (liver>plasma>kidney>heart>pancreas>brain ≈ CSF).

Chemical Information

CAS No. 3108258-69-8
Molecular Weight 440.45
Formula C₂₂H₂₄N₄O₆
SMILES

CC1=CC(CN2N=NN(C2=O)C3=CC4=C(OCCO4)C=C3)=CC(C)=C1OC(C)(C(O)=O)C
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]. Yao Y, et al. Discovery of Tetrazolone derivatives as potent PPARα/δ dual agonists for metabolic dysfunction-associated steatohepatitis. Bioorg Chem. 2026;175:109764. [Content Brief]

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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.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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PPARα/δ agonist 4

All PPAR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PPARα/δ agonist 4 Related Classifications

HY-183318 Related Classifications