PPARδ agonist 10
PPARδ agonist 10 (compound 7) is an orally active, selective, and partial agonist of PPARδ, with EC50 values of 0.053 μM and 0.30 µM for hPPARδ(LBD)-GAL4 and mPPARδ, respectively. PPARδ agonist 10 is a partial PPARδ agonist in transactivation assay but a full agonist on free fatty acids (FFA) oxidation in muscle cells both in vitro and in vivo. PPARδ agonist 10 can be used for dyslipidemia research.
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- CAS No.: 685139-10-0
- Formule: C23H17Br2ClO3S
- Masse moléculaire:568.71
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Activité biologique
Description
IC50 & Target
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PPARδ 0.053 μM (EC50, hPPARδ) |
PPARδ 0.30 μM (EC50, mPPARδ) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
>10 μM
Compound: 7
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Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay
Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay
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[PMID: 17343371] |
| HEK293 | EC50 |
>10 μM
Compound: 7
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Activity at human liver PPAR alpha expressed in HEK293 cells by PPAR-GAL4 transactivation assay
Activity at human liver PPAR alpha expressed in HEK293 cells by PPAR-GAL4 transactivation assay
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[PMID: 17343371] |
| HEK293 | EC50 |
0.053 μM
Compound: 7
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Activity at human placenta PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
Activity at human placenta PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
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[PMID: 17343371] |
| HEK293 | EC50 |
0.3 μM
Compound: 7
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Agonist activity at mouse PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
Agonist activity at mouse PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
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[PMID: 17343371] |
| L6 | EC50 |
30 nM
Compound: 7
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Effect on fatty acid oxidation in rat L6 cells
Effect on fatty acid oxidation in rat L6 cells
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[PMID: 17343371] |
In Vitro
PPARδ agonist 10 (compound 7) increases fatty acid oxidation in rat L6 muscle cells, with EC50 of 30 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PPARδ agonist 10 (5-20 mg/kg, PO, once daily) shows good oral pharmacokinetic properties in rat[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ApoB100/CETP-Tgn mice (female, 9-11 weeks old, with a mean body weight of 19.2 g±1.4, n=8/group, were fed a high fat diet)[1]
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Dosage:5, 10, and 20 mg/kg
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Administration:PO, once daily, for 6 weeks
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Result:Changed plasma lipid parameters in a dose-dependent manner to a less atherogenic profile, with increased HDL and decreased LDL and TG. HbA1c levels were lowered.
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Animal Model:Male SD rats[1]
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Dosage:1.06 mg/kg (IV)/2.06 mg/kg (PO)
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Administration:p.o. and i.v., single (Pharmacokinetic Analysis)
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Result:Pharmacokinetic Parameters of PPARδ agonist 10 in male Sprague-Dawley rats[1].
IV (1.06 mg/kg) PO (2.06 mg/kg) Cmax (ng/mL) 508 AUC0-24 (ng/mL∗min) 79294 t1/2 (min) 59 CL (mL/min/kg) 11.9 Vd, ss (L/kg) 0.3 F (%) 46%