1. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  2. PPAR
  3. GW7647

GW7647 is a potent PPARα agonist, with EC50s of 6 nM, 1.1 μM, and 6.2 μM for human PPARα, PPARγ and PPARδ, respectively.

For research use only. We do not sell to patients.

GW7647 Chemical Structure

GW7647 Chemical Structure

CAS No. : 265129-71-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 19 publication(s) in Google Scholar

Top Publications Citing Use of Products

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

GW7647 is a potent PPARα agonist, with EC50s of 6 nM, 1.1 μM, and 6.2 μM for human PPARα, PPARγ and PPARδ, respectively.

IC50 & Target[5]

PPARα

6 nM (EC50, Human PPARα)

PPARγ

1.1 μM (EC50, Human PPARγ)

PPARδ

6.2 μM (EC50, Human PPARδ)

Cellular Effect
Cell Line Type Value Description References
COS-7 EC50
0.2 μM
Compound: GW7647
Transactivation of human PPARalpha expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter gene assay
Transactivation of human PPARalpha expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter gene assay
[PMID: 26595749]
COS-7 EC50
0.2 μM
Compound: GW7647
Transactivation of GAL4-fused human PPARalpha ligand binding domain transfected in african green monkey COS7 cells by luciferase reporter gene assay
Transactivation of GAL4-fused human PPARalpha ligand binding domain transfected in african green monkey COS7 cells by luciferase reporter gene assay
[PMID: 23130964]
COS-7 EC50
0.23 μM
Compound: GW7647
Agonist activity at wild-type human PPARalpha LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
Agonist activity at wild-type human PPARalpha LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
[PMID: 25022880]
COS-7 EC50
0.23 μM
Compound: GW-7647
Transactivation of human PPARalpha LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay
Transactivation of human PPARalpha LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay
[PMID: 20307981]
COS-7 EC50
0.25 μM
Compound: GW7647
Agonist activity at wild-type human PPARalpha Thr279Ala mutant expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
Agonist activity at wild-type human PPARalpha Thr279Ala mutant expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
[PMID: 25022880]
HEK293 EC50
0.021 μM
Compound: GW7647
Agonist activity at N-terminal Gal4 fused human PPARalpha LBD transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay
Agonist activity at N-terminal Gal4 fused human PPARalpha LBD transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay
[PMID: 27622746]
HEK293 EC50
0.021 μM
Compound: GW7647
Agonist activity at GAL4-tagged human PPARalpha ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay
Agonist activity at GAL4-tagged human PPARalpha ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay
[PMID: 27591006]
HEK293 EC50
0.026 μM
Compound: GW7647
Agonist activity at GAL4N fused human PPARalpha LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay
Agonist activity at GAL4N fused human PPARalpha LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay
[PMID: 28539218]
HEK293 EC50
0.2 μM
Compound: 3, GW7647
Transactivation of human GAL4-fused PPARalpha ligand binding domain transfected in HEK293 cells after 18 hrs by dual luciferase reporter gene assay
Transactivation of human GAL4-fused PPARalpha ligand binding domain transfected in HEK293 cells after 18 hrs by dual luciferase reporter gene assay
[PMID: 23102891]
HEK293 EC50
0.2 μM
Compound: GW-7647
Agonist activity at Gal4-fused PPARalpha expressed in HEK293 cells after 18 hrs by dual luciferase reporter gene assay
Agonist activity at Gal4-fused PPARalpha expressed in HEK293 cells after 18 hrs by dual luciferase reporter gene assay
[PMID: 21889235]
HEK293 EC50
0.2 μM
Compound: GW-7647
Agonist activity at PPARalpha ligand binding domain expressed in HEK293 cells co-expressing GAL4 after 18 hrs by dual-luciferase activity based transactivation assay
Agonist activity at PPARalpha ligand binding domain expressed in HEK293 cells co-expressing GAL4 after 18 hrs by dual-luciferase activity based transactivation assay
[PMID: 21742490]
HEK293 EC50
0.2 μM
Compound: 1, GW-7647
Agonist activity at human PPARalpha expressed in HEK293 cells assessed as receptor transactivation at by luciferase reporter gene assay
Agonist activity at human PPARalpha expressed in HEK293 cells assessed as receptor transactivation at by luciferase reporter gene assay
[PMID: 19791744]
HEK293 IC50
0.46 nM
Compound: GW7647
Agonist activity at PPARalpha-LBD expressed in HEK293 cells co-expressing GAL4-DBD after 16 to 19 hrs by beta lactamase reporter gene assay
Agonist activity at PPARalpha-LBD expressed in HEK293 cells co-expressing GAL4-DBD after 16 to 19 hrs by beta lactamase reporter gene assay
[PMID: 22939697]
HEK293 EC50
0.6 nM
Compound: GW7647
Activation of PPARalpha transfected in HEK293 cells after 18 hrs by firefly luciferase reporter gene-based luminescence assay relative to control
Activation of PPARalpha transfected in HEK293 cells after 18 hrs by firefly luciferase reporter gene-based luminescence assay relative to control
[PMID: 21800856]
HEK293 EC50
0.89 nM
Compound: GW7647
Agonist activity at human PPARalpha expressed in HEK293 cells by luciferase reporter gene assay
Agonist activity at human PPARalpha expressed in HEK293 cells by luciferase reporter gene assay
[PMID: 25305688]
HEK293 EC50
13.6 nM
Compound: GW7647
Agonist activity at PPAR-alpha (unknown origin) expressed in HEK293 cells by luciferase reporter gene assay
Agonist activity at PPAR-alpha (unknown origin) expressed in HEK293 cells by luciferase reporter gene assay
[PMID: 24856059]
HEK293 EC50
7.1 nM
Compound: GW7647
Agonist activity at PPAR-alpha (unknown origin) expressed in HEK293 cells by TR-FRET assay
Agonist activity at PPAR-alpha (unknown origin) expressed in HEK293 cells by TR-FRET assay
[PMID: 24856059]
HEK293-A EC50
0.2 μM
Compound: 8, GW7674
Transactivation of PPARalpha expressed in HEK293A cells co-expressing GAL4 after 16 to 18 hrs by luciferase reporter gene assay
Transactivation of PPARalpha expressed in HEK293A cells co-expressing GAL4 after 16 to 18 hrs by luciferase reporter gene assay
[PMID: 23137448]
HEK-293T EC50
15.4 nM
Compound: GW7647
Agonist activity at GAL4-tagged PPARalpha ligand-binding domain (unknown origin) expressed in HEK293T cells incubated for 16 to 19 hrs by beta-lactamase reporter gene assay
Agonist activity at GAL4-tagged PPARalpha ligand-binding domain (unknown origin) expressed in HEK293T cells incubated for 16 to 19 hrs by beta-lactamase reporter gene assay
[PMID: 25491112]
MCF7 EC50
178 nM
Compound: GW-7647
Agonist activity at human PPARalpha expressed in human MCF7 cells coexpressing TIF2 by luciferase reporter gene assay
Agonist activity at human PPARalpha expressed in human MCF7 cells coexpressing TIF2 by luciferase reporter gene assay
[PMID: 18952442]
MCF7 EC50
6.5 nM
Compound: GW7647
Agonist activity at human PPARalpha transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay
Agonist activity at human PPARalpha transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay
[PMID: 26226490]
In Vitro

GW7647 (1 μM) causes a significant increase of PDZK1 protein expression to 129.7 ± 6.5% of vehicle treated control in Caco2BBE cells in the absence and presence of IL-1β. GW7647 also attenuates the IL-1β-mediated decrease in PDZK1 expression[1].
GW7647 (50 nM) stimulates the PI3K phosphorylation followed by the Akt (Ser473) phosphorylation, which induces NOS1 phosphorylation increased the amounts of NO released in the stripped antral mucosa. GW7647 (50 nM) enhances the initial phase of Ca2+-regulated exocytotic events stimulated by ACh in antral mucous cells, but GW7647 alone does not evoke any exocytotic event. GW7647 plus ACh stimulates the effects of wortmannin (50 nM) and AKT-inh (100 nM) on the exocytotic events in antral mucous cells[2].
GW 7647 (100 nM) reduces the AQP9 protein abundance by 43%, but it shows not significant effect at 10 and 1,000 nM in WIF-B9 hepatocytes. GW 7647 (100 nM) causes a 24% reduction in AQP9 protein abundance in HepG2 cells, however, it does not significantly increase the protein abundance of L-FABP in HepG2 hepatocytes[3].

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

In Vivo

GW7647 (3 mg/kg per day) does not prevent the development of cardiac hypertrophy, but it prevents the decline in left ventricular ejection fraction in vivo[4].

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

Molecular Weight

502.75

Formula

C29H46N2O3S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)(SC1=CC=C(CCN(C(NC2CCCCC2)=O)CCCCC3CCCCC3)C=C1)C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 60 mg/mL (119.34 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9891 mL 9.9453 mL 19.8906 mL
5 mM 0.3978 mL 1.9891 mL 3.9781 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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V1

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.97 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.97 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.45%

References
Animal Administration
[4]

Newborn New Zealand White rabbits of either sex (7 days old, 90-200 g) are anesthetized with inhaled isofluorane (2%), and are subjected to an aorto-caval shunt to induce volume-overload cardiac hypertrophy. The presence of a successful fistula is verified at postsurgical days 7 and 13 by color flow doppler that visualizes a physical shunt between the abdominal aorta and the inferior vena cava in both an axial and transverse plane. This is further validated by an enlarged inferior vena cava. After validation, the animals in shunt group are randomly assigned to receive an intraperitoneal injection of vehicle (dimethyl sulfoxide, the solvent of GW7647) or GW7647 (3 mg/kg per day; EC50=6 nM for PPARα) twice a day for 14 days. Animals that undergo surgery to create shunt, but consequently the shunt either not exhibiting or closed, are excluded from the study. Left ventricular ejection fraction (%) and other cardiac parameters are assessed by transthoracic echocardiography at postsurgical days 7 and 13. At 21 days of age (14 days post surgery), all animals are euthanized with Na+ pentobarbital, and hearts are removed for isolated biventricular working heart perfusions.

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

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9891 mL 9.9453 mL 19.8906 mL 49.7265 mL
5 mM 0.3978 mL 1.9891 mL 3.9781 mL 9.9453 mL
10 mM 0.1989 mL 0.9945 mL 1.9891 mL 4.9727 mL
15 mM 0.1326 mL 0.6630 mL 1.3260 mL 3.3151 mL
20 mM 0.0995 mL 0.4973 mL 0.9945 mL 2.4863 mL
25 mM 0.0796 mL 0.3978 mL 0.7956 mL 1.9891 mL
30 mM 0.0663 mL 0.3315 mL 0.6630 mL 1.6576 mL
40 mM 0.0497 mL 0.2486 mL 0.4973 mL 1.2432 mL
50 mM 0.0398 mL 0.1989 mL 0.3978 mL 0.9945 mL
60 mM 0.0332 mL 0.1658 mL 0.3315 mL 0.8288 mL
80 mM 0.0249 mL 0.1243 mL 0.2486 mL 0.6216 mL
100 mM 0.0199 mL 0.0995 mL 0.1989 mL 0.4973 mL
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GW7647
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