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

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PPARα/δ agonist 4

PPARα/δ agonist 4 Chemical Structure

CAS No. : 3108258-69-8

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PPARα/δ agonist 4 Related Antibodies

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Description

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[1].

IC50 & Target[1]

PPARα

0.36 nM (EC50)

PPARδ

1.31 nM (EC50)

PPARγ

160.84 nM (EC50)

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.

PPARα/δ agonist 4 Related Antibodies

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 T1/2 Tmax Cmax AUC0-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).
Molecular Weight

440.45

Formula

C22H24N4O6
CAS No.
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
References
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PPARα/δ agonist 4 Related Classifications

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  • 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/δ agonist 43108258-69-8PPARPeroxisome proliferator-activated receptorsPPARδmale SD ratsPPARγHepG2 cellsPPARαhERG channelACADVLbeagle dogsCPT1APDK4Inhibitorinhibitorinhibit

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