2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR
  4. GW0742

GW0742 is a potent PPARβ and PPARδ agonist, with an IC50 of 1 nM for human PPARδ in binding assay, and EC50s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ, respectively.

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GW0742 Chemical Structure

GW0742 Chemical Structure

CAS No. : 317318-84-6

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Customer Review

Based on 15 publication(s) in Google Scholar

GW0742 Related Antibodies

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View All PPAR Isoform Specific Products:

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PPARα PPARβ/δ PPARγ PPAR PPARδ

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

GW0742 is a potent PPARβ and PPARδ agonist, with an IC50 of 1 nM for human PPARδ in binding assay, and EC50s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ, respectively.

IC50 & Target[1]

PPARδ

1 nM (EC50)

PPARα

1.1 μM (EC50)

PPARγ

2 μM (EC50)

Cellular Effect
Cell Line Type Value Description References
CV-1 EC50
≤ 5.8 nM
Compound: GW-0742
Agonist activity at mouse PPAR-delta expressed in african green monkey CV-1 cells after 24 hrs by luciferase reporter gene assay
Agonist activity at mouse PPAR-delta expressed in african green monkey CV-1 cells after 24 hrs by luciferase reporter gene assay
[PMID: 21074432]
HEK293 EC50
13 nM
Compound: GW0742
Transactivation of GAL4-fused human PPARdelta LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay
Transactivation of GAL4-fused human PPARdelta LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay
[PMID: 30605833]
In Vitro

GW0742 is a potent PPARβ and PPARδ agonist, with an IC50 of 1 nM for human PPARδ, and EC50s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ respectively[1]. GW0742 (100 μM) activates human PPARα and mouse PPARβ in MCF-7 cells. GW0742 (100 μM) significantly reduces low-KCl-induced apoptosis of cerebellar granule neurons. GW0742 shows no obvious inherent toxicity on cerebellar granule neuronal cells after treatment of 3-100 μM for 24 h, but induces increased cell death at 100 μM after 48 hr of treatment. Moreover, GW0742 (100 μM) increases c-Jun expression in cerebellar granule neuron cultures observed at 6 hr[2]. GW0742 (1 μM) induces PPARδ protein in neonatal rat cardiomyocytes. GW0742 also raises mRNA levels of long-chain acyl-CoA dehydrogenase (LCAD), very long-chain acyl-CoA dehydrogenase (VLCAD), acyl-CoA oxidase 1 (ACOX1), uncoupling protein 3 (UCP3), malonyl-CoA decarboxylase (MCD), and pyruvate dehydrogenase kinase 4 (PDK4) in neonatal rat cardiomyocytes[4].

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

GW0742 Related Antibodies
In Vivo

GW0742 (0.3 mg/kg, i.p.) reduces intensity masson-trichrome staining, and attenuates the histological signs in bleomycin instillatio (BLEO)-induced lung injury of mice. GW0742 (0.3 mg/kg, i.p.) also causes a reduction of the BLEO-induced loss body weight, and a decrease of myeloperoxidase (MPO) activity. GW0742 shows significant inhibition of TNF-a and IL-1β in instilled-mice. GW0742 prevents bleomycin-induced IkB-a degradation, reduces the levels of NF-kB p65 in the lung, and decreases iNOS and p-ERK expression in BLEO-induced mice[3]. GW0742 (5 mg/kg/day, i.v.) increases PPARδ protein level in the heart of rats. GW0742 also induces the increase in LCAD, VLCAD, and ACOX1 in the heart of rats[4].

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

471.49

Formula

C21H17F4NO3S2
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(O)COC1=CC=C(SCC2=C(C)N=C(C3=CC=C(C(F)(F)F)C(F)=C3)S2)C=C1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 34 mg/mL (72.11 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 2.1209 mL 10.6047 mL 21.2094 mL
5 mM 0.4242 mL 2.1209 mL 4.2419 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

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 (5.30 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 (5.30 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:
%
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: 99.94%

SDS (393 KB)

COA (246 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[2]

The PPARβ activator GW0742 and the RXR activator 9-cis-retinoic acid are dissolved in DMSO. The final DMSO concentration des not exceed 0.5% v/v, and this concentration is used in control wells. For each culture plate, one row of wells is treated with 500 μM glutamate. These wells serve as a positive control and for normalisation of data. Cell death (toxicity) is assessed by using an assay designed to measure lactate dehydrogenase (LDH) release[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Male CD mice (25-35 g) are housed in a controlled environment and provided with standard rodent chow and water. Mice are randomized into four experimental groups: bleomycin-treated group: mice are subjected to lung injury induced by intratracheal instillation of bleomycin and treated daily via intraperitoneal injection with vehicle of GW0742 (10% dimethylsulfoxide (OMSO, 1 mL/kg), 1 h after BLEO instillation (n = 15). GW0742 group: identical to bleomycin-treated group but mice are treated daily with GW0742 (0.3 mg/kg, 1h after BLEO instillation) via intraperitoneal injection (n = 15). Sham-operated mice + vehicle group: animals are subjected to the identical surgical procedure but receive intratracheal instillation of saline (0.9%) instead of BLEO and are treated daily with the vehicle of GW0742 (10% dimethylsulfoxide (DMSO), 1 mL/kg, i.p.), 1 h after saline instillation (n = 15). Sham-operated mice + GW0742 group: identical to sham + vehicle group but mice are treated daily with GW0742 (0.3 mg/kg, 1 h after saline instillation) via intraperitoneal injection (n = 15)[3].

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1209 mL 10.6047 mL 21.2094 mL 53.0234 mL
5 mM 0.4242 mL 2.1209 mL 4.2419 mL 10.6047 mL
10 mM 0.2121 mL 1.0605 mL 2.1209 mL 5.3023 mL
15 mM 0.1414 mL 0.7070 mL 1.4140 mL 3.5349 mL
20 mM 0.1060 mL 0.5302 mL 1.0605 mL 2.6512 mL
25 mM 0.0848 mL 0.4242 mL 0.8484 mL 2.1209 mL
30 mM 0.0707 mL 0.3535 mL 0.7070 mL 1.7674 mL
40 mM 0.0530 mL 0.2651 mL 0.5302 mL 1.3256 mL
50 mM 0.0424 mL 0.2121 mL 0.4242 mL 1.0605 mL
60 mM 0.0353 mL 0.1767 mL 0.3535 mL 0.8837 mL
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GW0742 Related Classifications

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:

GW0742317318-84-6GW610742GW 0742GW-0742GW 610742GW-610742PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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