2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR
  4. 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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PPARδ agonist 10 Chemical Structure

PPARδ agonist 10 Chemical Structure

CAS No. : 685139-10-0

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PPARδ agonist 10 Related Antibodies

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Description

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[1].

IC50 & Target

PPARδ

0.053 μM (EC50, hPPARδ)

PPARδ

0.30 μM (EC50, mPPARδ)

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
> 10 μM
Compound: 7
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
[PMID: 17343371]
HEK293 EC50
> 10 μM
Compound: 7
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
[PMID: 17343371]
HEK293 EC50
0.053 μM
Compound: 7
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
[PMID: 17343371]
HEK293 EC50
0.3 μM
Compound: 7
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
[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.

PPARδ agonist 10 Related Antibodies
In Vivo

PPARδ agonist 10 (compound 7) changes plasma lipid parameters in a dose-dependent manner to a less atherogenic profile[1].
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.

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]
Dosage: 5, 10, and 20 mg/kg
Administration: PO, once daily, for 6 weeks
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.
Animal Model: Male SD rats[1]
Dosage: 1.06 mg/kg (IV)/2.06 mg/kg (PO)
Administration: p.o. and i.v., single (Pharmacokinetic Analysis)
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%
Molecular Weight

568.71

Formula

C23H17Br2ClO3S
CAS No.
SMILES

O=C(COC1=CC=C(C=C1Cl)SC/C=C(C2=CC=C(C=C2)Br)/C3=CC=C(C=C3)Br)O
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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PPARδ agonist 10 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:

PPARδ agonist 10685139-10-0PPARδ agonist10PPARδ agonist-10PPARPeroxisome proliferator-activated receptorsrat muscle L6 cellatherogenicdyslipidemiaInhibitorinhibitorinhibit

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