Art. -Nr.: HY-15577

GSK3787

17 Cited Publications

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Based on 17 publication(s) in Google Scholar

GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC₅₀ of 6.6.

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Reinheit: 99.94%
CAS. Nr.: 188591-46-0
Formel: C₁₅H₁₂ClF₃N₂O₃S
Molecular Weight:392.78

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GSK3787 Chemical Structure

CAS. Nr.: 188591-46-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (17)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC₅₀ of 6.6.

IC₅₀ & Target^[1]

PPARδ

6.6 nM (pIC₅₀)

Alle PPAR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
COS-1	IC₅₀	5 μM Compound: 9, GSK3787	Antagonist activity against pSG5-Gal4-tagged human PPAR-beta/delta ligand binding domain expressed in COS1 cells assessed as inhibition of GW501516-induced receptor activation incubated for 19 hrs by pGL3-5XUAS-SV40 luciferase reporter gene assay Antagonist activity against pSG5-Gal4-tagged human PPAR-beta/delta ligand binding domain expressed in COS1 cells assessed as inhibition of GW501516-induced receptor activation incubated for 19 hrs by pGL3-5XUAS-SV40 luciferase reporter gene assay	[PMID: 25768705]

In Vitro

GSK3787 is identified as a potent and selective hPPARδ ligand (pIC₅₀=6.6) with no measurable affinity for hPPARα or hPPARγ (pIC₅₀ < 5) in our standard in vitro ligand displacement assay. GSK3787 is inactive against hPPARα and hPPARγ in similar functional antagonist assays. GSK3787 fails to activate the receptor in a standard hPPARδ-GAL4 chimera cell-based reporter assay. GSK3787 is a selective PPARδ antagonist with equipotent species activity against the human and mouse receptor^[1].

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

In Vivo

GSK3787 has pharmacokinetic properties suitable for use as an in vivo PPARδ antagonist tool compound in mice. GSK3787 is administered intravenously (0.5 mg/kg) and orally (10 mg/kg) to male C57BL/6 mice. Mean clearance (CL) and volume of distribution at steady state (V_ss) following iv administration are 39±11 (mL/min)/kg and 1.7±0.4 L/kg, respectively. Following oral administration, good exposure (C_max=881±166 ng/mL, AUC_inf=3343±332 h•ng/mL), half-life (2.7±1.1 h), and bioavailability (F=77±17%) are observed^[1]. Oral administration of GSK3787 (10 mg/kg) leads to a serum C_max of 2.2±0.4 μM in C57BL/6 male mice. Oral administration of GW0742 causes an increase in expression of Angptl4 and Adrp mRNA (known PPARβ/δ target genes) in wild-type mouse colon epithelium, and this effect is not found in Pparβ/δ-null mouse colon epithelium. Coadministration of GSK3787 with GW0742 effectively prevents the ligand-induced expression of both Angptl4 and Adrp mRNA in wild-type mouse colon epithelium, and this effect is not found in Pparβ/δ-null mouse colon epithelium. Oral administration of GSK3787 causes a modest increase in promoter occupancy of PPARβ/δ in the PPRE region of both the Angptl4 and Adrp genes, but coadministration of GSK3787 with GW0742 results in markedly less accumulation of PPARβ/δ in the PPRE region of both the Angptl4 and Adrp genes in wild-type mouse colon epithelium^[2].

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

Chemical Information

CAS. Nr. 188591-46-0
Appearance Solid
Molecular Weight 392.78
Formel C₁₅H₁₂ClF₃N₂O₃S
Color White to off-white
SMILES

O=C(NCCS(=O)(C1=NC=C(C(F)(F)F)C=C1)=O)C2=CC=C(Cl)C=C2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (17)

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Journal Impact Factor

Nat Commun

Selective inhibition of cancer cell self-renewal through a Quisinostat-histone H1.0 axis. [Abstract]

2020 Apr 14;11(1):1792. PMID: 32286289
Cell Death Dis

CILP1 interacting with YBX1 promotes hypertrophic scar formation by suppressing PPARs transcription. [Abstract]

2025 May 9;16(1):371. PMID: 40346063
Biol Psychiatry

Transcription Factor TWIST1 Integrates Dendritic Remodeling and Chronic Stress to Promote Depressive-like Behaviors. [Abstract]

2021 Mar 15;89(6):615-626. PMID: 33190845
Food Res Int

Fisetin, a dietary flavonoid, promotes transintestinal cholesterol excretion through the activation of PPARδ. [Abstract]

2024 Jan:175:113783. PMID: 38129008
Int J Biol Macromol

Visceral obesity-induced METTL27 regulation of the FABP5/PPARD/CPT1A axis in promoting colorectal cancer progression. [Abstract]

2026 Feb:347:150740. PMID: 41651272
Cell Rep

Lipid accumulation-mediated histone hypoacetylation drives persistent NK cell dysfunction in anti-tumor immunity. [Abstract]

2023 Oct 3;42(10):113211. PMID: 37792534
Environ Pollut

Perturbation of IP3R-dependent endoplasmic reticulum calcium homeostasis by PPARδ-activated metabolic stress leads to mouse spermatocyte apoptosis: A direct mechanism for perfluorooctane sulfonic acid-induced spermatogenic disorders. [Abstract]

2024 Feb 15:343:123167. PMID: 38110051
J Ethnopharmacol

Chrysanthemum morifolium Ramat. water extract prevents and treats metabolic-associated fatty liver disease via pan-PPAR activity. [Abstract]

2025 Sep 6;355(Pt A):120571. PMID: 40921229
Biomolecules

PPARs Activity Affects the Hatchability Through Lipid Metabolism Regulation in Silkworm, Bombyx mori L. [Abstract]

2025 Mar 27;15(4):492. PMID: 40305260
Front Pharmacol

PPARβ/δ Agonist GW501516 Inhibits Tumorigenicity of Undifferentiated Nasopharyngeal Carcinoma in C666-1 Cells by Promoting Apoptosis. [Abstract]

2018 Jun 28:9:648. PMID: 30002625
Toxics

Differential Disruption of Glucose and Lipid Metabolism Induced by Phthalates in Human Hepatocytes and White Adipocytes. [Abstract]

2024 Mar 14;12(3):214. PMID: 38535947
Cell Signal

CD137 signaling induces macrophage M2 polarization in atherosclerosis through STAT6/PPARδ pathway. [Abstract]

2020 Aug;72:109628. PMID: 32247042
Oncol Res

PPARβ/δ Agonist GW501516 Inhibits Tumorigenesis and Promotes Apoptosis of the Undifferentiated Nasopharyngeal Carcinoma C666-1 Cells by Regulating miR-206. [Abstract]

2019 Aug 8;27(8):923-933. PMID: 30982495
iScience

Excipient of paclitaxel induces metabolic dysregulation and unfolded protein response. [Abstract]

2021 Sep 25;24(10):103170. PMID: 34646996
Acta Biochim Biophys Sin (Shanghai)

AT1-receptor autoantibody exposure in utero contributes to cardiac dysfunction and increased glycolysis in fetal mice. [Abstract]

2020 Dec 29;52(12):1373-1381. PMID: 33231607
Nutrition

β-hydroxy-β-methylbutyrate (HMB) improves mitochondrial function in myocytes through pathways involving PPARβ/δ and CDK4. [Abstract]

2019 Apr:60:217-226. PMID: 30677545

GSK3787 purchased from MedChemExpress. Usage Cited in: Nutrition. 2019 Apr:60:217-226. [Abstract]

Leu and HMB stimulate the protein expression of PPARβ/δ and CDK4, and GSK3787 and LY2835219 block the protein expression of PPARβ/δ and CDK4.

GSK3787 purchased from MedChemExpress. Usage Cited in: Nutrition. 2019 Apr:60:217-226. [Abstract]

The mRNA expression levels of AMPKα, Sirt1, PGC-1α change significantly with the treatment of GSK3787 or LY2835219 are showed.

GSK3787 purchased from MedChemExpress. Usage Cited in: Nutrition. 2019 Apr:60:217-226. [Abstract]

The mRNA expression levels of Nrf-1, TFAM, MEF-2A, MEF-2CD, and MEF-2C change significantly with the treatment of GSK3787 or LY2835219 are showed.

GSK3787 purchased from MedChemExpress. Usage Cited in: Nutrition. 2019 Apr:60:217-226. [Abstract]

GSK3787 significantly reverse the beneficial effects of Leu and HMB on mitochondrial mass.
Sci Total Environ

PPARβ/δ-ANGPTL4 axis mediates the promotion of mono-2-ethylhexyl phthalic acid on MYCN-amplified neuroblastoma development. [Abstract]

2024 Feb 20:912:168949. PMID: 38042186

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 50 mg/mL (127.30 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5460 mL

12.7298 mL

25.4595 mL

5 mM

0.5092 mL

2.5460 mL

5.0919 mL

10 mM

0.2546 mL

1.2730 mL

2.5460 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 (6.36 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (6.36 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

Animal Administration^[2]

Mice^[2]
For RNA and DNA analysis, male wild-type and Pparβ/δ-null mice are administered vehicle (corn oil), GW0742 (10 mg/kg), GSK3787 (10 mg/kg), or GW0742 and GSK3787 by oral gavage 3 h before euthanasia. After euthanasia, colons are carefully dissected. To isolate colon epithelium, colons are flushed with phosphate-buffered saline, and epithelial cells are scraped from mucosa using a razor blade. The isolated tissues are used for RNA isolation. For glucose-tolerance tests, male wild-type and Pparβ/δ-null mice are administered vehicle (corn oil), GW0742 (10 mg/kg), GSK3787 (10 mg/kg), or Rosiglitazone (20 mg/kg) by oral gavage once a day for 2 weeks.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (289 KB)
SDS (537 KB)
- English - EN (537 KB)
- Français - FR (537 KB)
- Deutsch - DE (537 KB)
- Norwegian - NO (537 KB)
- Español - ES (537 KB)
- Swedish - SV (537 KB)
- Italian - IT (537 KB)
- Korean - KR (537 KB)
- Portuguese - PT (537 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Shearer BG, et al. Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist. J Med Chem. 2010 Feb 25;53(4):1857-61. [Content Brief]

[2]. Palkar PS, et al. Cellular and pharmacological selectivity of the peroxisome proliferator-activated receptor-beta/delta antagonist GSK3787. Mol Pharmacol. 2010 Sep;78(3):419-30. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.5460 mL	12.7298 mL	25.4595 mL	63.6489 mL
	5 mM	0.5092 mL	2.5460 mL	5.0919 mL	12.7298 mL
	10 mM	0.2546 mL	1.2730 mL	2.5460 mL	6.3649 mL
	15 mM	0.1697 mL	0.8487 mL	1.6973 mL	4.2433 mL
	20 mM	0.1273 mL	0.6365 mL	1.2730 mL	3.1824 mL
	25 mM	0.1018 mL	0.5092 mL	1.0184 mL	2.5460 mL
	30 mM	0.0849 mL	0.4243 mL	0.8487 mL	2.1216 mL
	40 mM	0.0636 mL	0.3182 mL	0.6365 mL	1.5912 mL
	50 mM	0.0509 mL	0.2546 mL	0.5092 mL	1.2730 mL
	60 mM	0.0424 mL	0.2122 mL	0.4243 mL	1.0608 mL
	80 mM	0.0318 mL	0.1591 mL	0.3182 mL	0.7956 mL
	100 mM	0.0255 mL	0.1273 mL	0.2546 mL	0.6365 mL

Keywords

GSK3787

17 Cited Publications

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GSK3787

Cell Cycle/DNA Damage Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-diabetic Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Mitochondrial Toxicity Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

RNA Binding Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GSK3787

Alle PPAR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (17)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GSK3787

Cell Cycle/DNA Damage Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-diabetic Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Mitochondrial Toxicity Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

RNA Binding Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GSK3787

Alle PPAR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (17)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GSK3787 Related Classifications

HY-15577 Related Classifications