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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- CAS. Nr.: 3056618-93-7
- Formel: C27H24F3N2NaO4
- Molecular Weight:520.48
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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PPARδ 0.5 nM (EC50) |
PPARα >10000 nM (EC50) |
PPARγ >10000 nM (EC50) |
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.
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Cell Line:Human renal proximal tubule HK2 cells
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Concentration:10, 100, 1000 nM
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Incubation Time:6 h
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Result:Dose-dependently upregulated the expression of PPARδ target genes ANGPTL4, PDK4, and CPT1A in HK2 cells.
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Cell Line:NRK-49F cells
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Concentration:2.5, 10 nM
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Incubation Time:23 h (after 1 h TGF-β1 pre-treatment)
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Result:Dose-dependently suppressed the TGF-β1-induced expression of fibrotic markers α-SMA and fibronectin in NRK-49F cells.
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.
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Animal Model:C57BL/6JNifdc (male, 7-8 weeks old, ~22 g, nilateral ureteral obstructio model)[1]
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Dosage:3 mg/kg; 10 mg/kg
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Administration:I.g.; daily; 13 days
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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.
Chemical Information
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CAS. Nr. 3056618-93-7
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Molecular Weight 520.48
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Formel C27H24F3N2NaO4
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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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
PPARδ agonist 13 Related Classifications
HY-181652 Related Classifications
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