GW7647

Name: GW7647
Brand: MedChemExpress
SKU: HY-13861
Rating: 5.0 (20 reviews)

Cat. No.: HY-13861 Purity: 99.45%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

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

CAS No. : 265129-71-3

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 20 publication(s) in Google Scholar

19 Publications Citing Use of MCE GW7647

: GW7647 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Oct;1864(10):3322-3338. [Abstract]; LAZ3 knock-down decreases NRF2 expression and nuclear translocation, while only the PPARa agonist (GW7647) can prevent this inhibition. Both PPARγ agonist (GW1929) and PPARδ agonist (GW0742) can not reverse these inhibitions.

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PPARα PPARβ/δ PPARγ PPAR PPARδ

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.

265129-71-3

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
10 mM	0.1989 mL	0.9945 mL	1.9891 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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:

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mg/kg

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(per animal)

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(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:

DMSO +

Tween-80 +

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%

Select Batch:

Data Sheet (282 KB) SDS (252 KB)

COA (250 KB) HNMR (287 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

References

[1]. Luo M, et al. IL-1β-Induced Downregulation of the Multifunctional PDZ Adaptor PDZK1 Is Attenuated by ERK Inhibition, RXRα, or PPARα Stimulation in Enterocytes. Front Physiol. 2017 Feb 7;8:61. [Content Brief]

[2]. Tanaka S, et al. PPARα induced NOS1 phosphorylation via PI3K/Akt in guinea pig antral mucous cells: NO-enhancement in Ca(2+)-regulated exocytosis. Biomed Res. 2016;37(3):167-78. [Content Brief]

[3]. Lebeck J, et al. Hepatic AQP9 expression in male rats is reduced in response to PPARα agonist treatment. Am J Physiol Gastrointest Liver Physiol. 2015 Feb 1;308(3):G198-205. [Content Brief]

[4]. Lam VH, et al. Activating PPARα prevents post-ischemic contractile dysfunction in hypertrophied neonatal hearts. Circ Res. 2015 Jun 19;117(1):41-51. [Content Brief]

[5]. Brown PJ, et al. Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis. Bioorg Med Chem Lett. 2001 May 7;11(9):1225-7. [Content Brief]

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

[1]. Luo M, et al. IL-1β-Induced Downregulation of the Multifunctional PDZ Adaptor PDZK1 Is Attenuated by ERK Inhibition, RXRα, or PPARα Stimulation in Enterocytes. Front Physiol. 2017 Feb 7;8:61. [Content Brief]

[2]. Tanaka S, et al. PPARα induced NOS1 phosphorylation via PI3K/Akt in guinea pig antral mucous cells: NO-enhancement in Ca(2+)-regulated exocytosis. Biomed Res. 2016;37(3):167-78. [Content Brief]

[3]. Lebeck J, et al. Hepatic AQP9 expression in male rats is reduced in response to PPARα agonist treatment. Am J Physiol Gastrointest Liver Physiol. 2015 Feb 1;308(3):G198-205. [Content Brief]

[4]. Lam VH, et al. Activating PPARα prevents post-ischemic contractile dysfunction in hypertrophied neonatal hearts. Circ Res. 2015 Jun 19;117(1):41-51. [Content Brief]

[5]. Brown PJ, et al. Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis. Bioorg Med Chem Lett. 2001 May 7;11(9):1225-7. [Content Brief]

Complete Stock Solution Preparation Table

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

GW7647 Related Classifications

Cardiovascular Disease

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:

GW7647265129-71-3GW 7647GW-7647PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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GW7647

Customer Review

GW7647 Related Antibodies

19 Publications Citing Use of MCE GW7647

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

GW7647 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GW7647 Related Classifications

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