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

PPAR agonist 4 (Compound 12) is an orally active agonist for peroxisome proliferator-activated receptor (PPAR), which activates PPARα, PPARδ and PPARγ with EC50s of 0.7, 0.7 and 1.8 μM, respectively. PPAR agonist 4 exhibits anti-liver fibrosis efficacy.

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PPAR agonist 4 Chemical Structure

PPAR agonist 4 Chemical Structure

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PPAR agonist 4 Related Antibodies

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Description

PPAR agonist 4 (Compound 12) is an orally active agonist for peroxisome proliferator-activated receptor (PPAR), which activates PPARα, PPARδ and PPARγ with EC50s of 0.7, 0.7 and 1.8 μM, respectively. PPAR agonist 4 exhibits anti-liver fibrosis efficacy[1].

IC50 & Target

PPARα

0.7 μM (EC50)

PPARδ

0.7 μM (EC50)

PPARγ

1.8 μM (EC50)

In Vitro

PPAR agonist 4 (3-10 μM) dose-dependently upregulates expressions of PPARα/δ target genes CPT1A, PDK4 and ANGPTL4 in HepG2 cells and PPARγ target genes CD36 and FABP4 in HEK293 cells[1].

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

PPAR agonist 4 Related Antibodies

RT-PCR[1]

Cell Line: HepG2 and HEK293
Concentration: 3-10 μM
Incubation Time: 12 h
Result: Upregulated levels of CPT1A, PDK4 and ANGPTL4, downregulated levels of CD36 and FABP4.
In Vivo

PPAR agonist 4 (3-30 mg/kg, p.o. for 3 weeks) ameliorates collagen deposition and suppressees inflammatory cell infiltration in the CCl4-induced liver fibrosis mouse model[1].

Pharmacokinetic Analysis of PPAR agonist 4 in Sprague-Dawley rats[1]

route Dose (mg/kg) T1/2 (h) MRT (h) Cmax (μM) AUC0-t (h·μM) F (%)
i.v. 2 9.7 6.8 12.2 59.8 -
p.o. 10 17.0 10.1 15.9 274.5 91.8

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

Animal Model: CCL4-induced liver fibrosis in C57BL/6 mice[1]
Dosage: 3-30 mg/kg
Administration: p.o., once a day for 3 weeks
Result: Reduced levels of collagen and α-SMA, reduced accumulation of collagen and inflammatory cell infiltration in the portal area.
Upregulated the expression of PPARs target genes (Cpt1a, Cpt2, Angptl4 and Cd36).
Molecular Weight

451.48

Formula

C23H28F3N3O3
SMILES

CC1=CC(CN2CCN(CC2)C3=NC=C(C=C3)C(F)(F)F)=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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PPAR agonist 4 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:

PPAR agonist 4PPAR agonist4PPAR agonist-4PPARPeroxisome proliferator-activated receptorsliver fibrosisSprague-Dawley ratsInhibitorinhibitorinhibit

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