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.
For research use only. We do not sell to patients.
- CAS No.: 685139-10-0
- Formula: C23H17Br2ClO3S
- Molecular Weight:568.71
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PPARδ 0.053 μM (EC50, hPPARδ) |
PPARδ 0.30 μM (EC50, mPPARδ) |
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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] |
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.
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%