2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR
  4. PPARδ agonist 13

PPARδ agonist 13 is a potent, selective and orally active PPARδ agonist with an EC50 values of 0.50 nM. PPARδ agonist 13 binds to the PPARδ ligand-binding pocket and upregulates PPARδ target gene expression. PPARδ agonist 13 inhibits renal fibroblast activation, restores fatty acid oxidation, and attenuates TGF-β1-induced renal fibroblast activation. PPARδ agonist 13 exhibits anti-renal fibrosis effects in a mouse model of unilateral ureteral obstruction. PPARδ agonist 13 can be used for the research of renal fibrosis.

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PPARδ agonist 13

PPARδ agonist 13 Chemical Structure

CAS No. : 3056618-93-7

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PPARδ agonist 13 Related Antibodies

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Description

PPARδ agonist 13 is a potent, selective and orally active PPARδ agonist with an EC50 values of 0.50 nM. PPARδ agonist 13 binds to the PPARδ ligand-binding pocket and upregulates PPARδ target gene expression. PPARδ agonist 13 inhibits renal fibroblast activation, restores fatty acid oxidation, and attenuates TGF-β1-induced renal fibroblast activation. PPARδ agonist 13 exhibits anti-renal fibrosis effects in a mouse model of unilateral ureteral obstruction. PPARδ agonist 13 can be used for the research of renal fibrosis[1].

IC50 & Target[1]

PPARδ

0.5 nM (EC50)

PPARα

>10000 nM (EC50)

PPARγ

>10000 nM (EC50)

In Vitro

PPARδ agonist 13 (Compound 16a) (10-1000 nM; 6 h) dose-dependently upregulates PPARδ target gene expression in HK2 cells[1].
PPARδ agonist 13 (0.2-5 μM; 16 h) shows high selectivity for PPARδ in Cos-7 cells, with only weak PPARγ agonism observed at the highest tested concentration of 5 μM[1].
PPARδ agonist 13 (1-30 μM; 3 min) directly interacts with purified PPARδ LBD protein, as demonstrated by dose-dependent reduction of ANS fluorescence[1].
PPARδ agonist 13 (0.3-30 μM) does not inhibit hERG potassium channels in hERG knock-in HEK293 cells, indicating low cardiovascular risk[1].
PPARδ agonist 13 (2.5-10 nM; 23 h) dose-dependently attenuates TGF-β1-induced activation of NRK-49F renal fibroblasts, reducing α-SMA and fibronectin expression at concentrations of 2.5 and 10 nM[1].

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

PPARδ agonist 13 Related Antibodies

RT-PCR[1]

Cell Line: Human renal proximal tubule HK2 cells
Concentration: 10, 100, 1000 nM
Incubation Time: 6 h
Result: Dose-dependently upregulated the expression of PPARδ target genes ANGPTL4, PDK4, and CPT1A in HK2 cells.

Western Blot Analysis[1]

Cell Line: NRK-49F cells
Concentration: 2.5, 10 nM
Incubation Time: 23 h (after 1 h TGF-β1 pre-treatment)
Result: Dose-dependently suppressed the TGF-β1-induced expression of fibrotic markers α-SMA and fibronectin in NRK-49F cells.
Parmacokinetics
Species Dose Route T1/2 Cmax AUC0-∞ CL F
Rat[1] 2 mg/kg i.v. 2.59 ± 0.79 h 44697 ± 13239 ng/mL 31986 ± 2943 ng·h/mL 0.06 ± 0.01 L/h/kg /
Rat[1] 10 mg/kg p.o. 2.60 ± 0.45 h 16133 ± 4332 ng/mL 69196 ± 14574 ng·h/mL 0.15 ± 0.04 L/h/kg 43 %
In Vivo

PPARδ agonist 13 (3-10 mg/kg; i.g.; daily; 13 days) dose-dependently ameliorates unilateral ureteral obstructio-induced renal fibrosis in male C57BL/6JNifdc mice via reducing fibrotic gene expression, inflammation, apoptosis, and restoring fatty acid oxidation pathways[1].
PPARδ agonist 13 (100 mg/kg for 14 days or 2000 mg/kg single dose; i.g.) shows low toxicity in C57BL/6JNifdc mice[1].

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

Animal Model: C57BL/6JNifdc (male, 7-8 weeks old, ~22 g, nilateral ureteral obstructio model)[1]
Dosage: 3 mg/kg; 10 mg/kg
Administration: I.g.; daily; 13 days
Result: Relieved UUO-induced tubular atrophy and dilation.
Significantly reduced UUO-induced collagen accumulation and decreased protein expression of collagen I and collagen III.
Potently downregulated UUO-induced upregulation of α-SMA protein levels and mRNA expression of fibrotic genes (Acta2, Col1a1, Col3a1, Col4a1, Fn1, Vim, Tgfb1, Ctgf).
Reduced UUO-induced renal interstitial inflammatory cell infiltration and dose-dependently suppressed elevated mRNA levels of pro-inflammatory cytokines/chemokines (Tnf, Il1b, Il6, Ccl4, Ccl5).
Decreased protein levels of phosphorylated NF-κB p65 and phosphorylated JNK, and increased the antiapoptotic Bcl-2 to pro-apoptotic Bax protein ratio to mitigate UUO-induced renal apoptosis.
Dose-dependently restored UUO-downregulated mRNA expression of fatty acid oxidation-related genes (Cpt1a, Cpt2, Acadm, Acadvl, Acads, Ppargc1a) in kidney tissue.
Molecular Weight

520.48

Formula

C27H24F3N2NaO4
CAS No.
SMILES

O=C(CCCCCOC1=C(CN2C(C3=CC=C(C=C3)OC(F)(F)F)=NC4=C2C=CC=C4)C=CC=C1)O[Na]
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Purity & Documentation
References
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PPARδ agonist 13 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:

PPARδ agonist 133056618-93-7PPARδ agonist13PPARδ agonist-13PPARPeroxisome proliferator-activated receptorsPPARδCos-7 cellsNRK-49F renal fibroblastsrenal fibroblastrenal fibrosismouse model of unilateral ureteral obstructionHK2 cellshERG knock-in HEK293 cellsPPARδ ligand-binding pocketTGF-β1Inhibitorinhibitorinhibit

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