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GW 501516

(Synonyms: GW 1516; GSK-516)

29 Cited Publications

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Based on 29 publication(s) in Google Scholar

GW 501516 (GW 1516) is a PPARδ agonist with an EC₅₀ of 1.1 nM.

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Pureté: 99.27%
CAS No.: 317318-70-0
Formule: C₂₁H₁₈F₃NO₃S₂
Masse moléculaire:453.50

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GW 501516 Chemical Structure

CAS No.: 317318-70-0

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (29)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

GW 501516 (GW 1516) is a PPARδ agonist with an EC₅₀ of 1.1 nM^[1].

IC₅₀ & Target^[1]

PPARδ

1.1 nM (EC₅₀)

Voir tous les produits spécifiques à Isoform PPAR :

Cellular Effect

Cell Line	Type	Value	Description	References
COS-1	EC₅₀	2.9 nM Compound: 1, GW-501516	Agonist activity at human PPARdelta ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis Agonist activity at human PPARdelta ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis	[PMID: 22051054]
COS-1	EC₅₀	912 nM Compound: 1, GW-501516	Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis	[PMID: 22051054]
COS-1	EC₅₀	>1000 nM Compound: 1, GW-501516	Agonist activity at human PPARalpha ligand binding domain expressed in COS-1 cells co-transfected with Gal4 after 24 hrs by luciferase reporter gene assay Agonist activity at human PPARalpha ligand binding domain expressed in COS-1 cells co-transfected with Gal4 after 24 hrs by luciferase reporter gene assay	[PMID: 22051054]
COS-1	EC₅₀	0.5 nM Compound: 1, GW501516	Agonist activity at pSG5-Gal4-tagged human PPAR-beta/delta ligand binding domain expressed in COS1 cells assessed as receptor activation incubated for 19 hrs by pGL3-5XUAS-SV40 luciferase reporter gene assay Agonist activity at pSG5-Gal4-tagged human PPAR-beta/delta ligand binding domain expressed in COS1 cells assessed as receptor activation incubated for 19 hrs by pGL3-5XUAS-SV40 luciferase reporter gene assay	[PMID: 25768705]
COS-7	EC₅₀	1 nM Compound: GW-501516	Activity at PPARbeta/delta by luciferase reporter gene transactivation assay in COS7 cells Activity at PPARbeta/delta by luciferase reporter gene transactivation assay in COS7 cells	[PMID: 16797985]
COS-7	EC₅₀	10000 nM Compound: GW-501516	Activity at PPARgamma by luciferase reporter gene transactivation assay in COS7 cells Activity at PPARgamma by luciferase reporter gene transactivation assay in COS7 cells	[PMID: 16797985]
COS-7	EC₅₀	10 μM Compound: GW-501516	Activity at PPARalpha by luciferase reporter gene transactivation assay in COS7 cells Activity at PPARalpha by luciferase reporter gene transactivation assay in COS7 cells	[PMID: 16797985]
CV-1	EC₅₀	0.001 μM Compound: 1, GW-501516	Agonist potency at PPARdelta in CV1 cells by cell based transient transfection assay Agonist potency at PPARdelta in CV1 cells by cell based transient transfection assay	[PMID: 17243659]
CV-1	EC₅₀	1.888 μM Compound: 1, GW-501516	Agonist potency at PPARalpha in CV1 cells by cell based transient transfection assay Agonist potency at PPARalpha in CV1 cells by cell based transient transfection assay	[PMID: 17243659]
CV-1	EC₅₀	8.9 μM Compound: 1, GW-501516	Agonist potency at PPARgamma in CV1 cells by cell based transient transfection assay Agonist potency at PPARgamma in CV1 cells by cell based transient transfection assay	[PMID: 17243659]
CV-1	EC₅₀	0.0017 μM Compound: GW-501516	Transactivation of Gal4-fused human PPARdelta DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay Transactivation of Gal4-fused human PPARdelta DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay	[PMID: 21112784]
CV-1	EC₅₀	0.99 μM Compound: GW-501516	Transactivation of Gal4-fused human PPARalpha DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay Transactivation of Gal4-fused human PPARalpha DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay	[PMID: 21112784]
CV-1	EC₅₀	4.1 μM Compound: GW-501516	Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay	[PMID: 21112784]
CV-1	EC₅₀	0.0017 μM Compound: 1, GW-501516	Agonist activity at human PPARdelta-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay Agonist activity at human PPARdelta-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay	[PMID: 21515063]
CV-1	EC₅₀	0.99 μM Compound: 1, GW-501516	Agonist activity at human PPARalpha-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay Agonist activity at human PPARalpha-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay	[PMID: 21515063]
CV-1	EC₅₀	4.1 μM Compound: 1, GW-501516	Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay	[PMID: 21515063]
CV-1	EC₅₀	>1.2 μM Compound: GW501516	Transactivation activity at human PPARgamma expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay Transactivation activity at human PPARgamma expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay	[PMID: 22534184]
CV-1	EC₅₀	2.5 nM Compound: GW501516	Transactivation activity at human PPARdelta expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay Transactivation activity at human PPARdelta expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay	[PMID: 22534184]
CV-1	EC₅₀	229 nM Compound: GW501516	Transactivation activity at human PPARalpha expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay Transactivation activity at human PPARalpha expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay	[PMID: 22534184]
CV-1	EC₅₀	0.0012 μM Compound: GW501516	Transactivation of human PPARdelta expressed in african green monkey CV1 cells by luciferase reporter gene assay Transactivation of human PPARdelta expressed in african green monkey CV1 cells by luciferase reporter gene assay	[PMID: 22579420]
HEK293	EC₅₀	>10 μM Compound: GW-501516	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	0.0079 μM Compound: GW-501516	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	0.054 μM Compound: GW-501516	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]
HEK293	EC₅₀	3.9 μM Compound: GW-501516	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	0.085 μM Compound: GW-501516	Agonist activity at human PPARdelta receptor expressed in HEK293 cells by GAL4 transactivation assay Agonist activity at human PPARdelta receptor expressed in HEK293 cells by GAL4 transactivation assay	[PMID: 17524643]
HEK293	EC₅₀	1.8 nM Compound: GW-501516	Effect on PPARdelta transactivation activity in HEK293 cells Effect on PPARdelta transactivation activity in HEK293 cells	[PMID: 17532641]
HEK293	EC₅₀	8600 nM Compound: GW-501516	Effect on PPARgamma transactivation activity in HEK293 cells Effect on PPARgamma transactivation activity in HEK293 cells	[PMID: 17532641]
HEK293	EC₅₀	1 μM Compound: GW-501516	Effect on PPARalpha transactivation activity in HEK293 cells Effect on PPARalpha transactivation activity in HEK293 cells	[PMID: 17532641]
HEK293	EC₅₀	0.002 μM Compound: 1, GW-501516	Agonist activity at Gal4-fused human PPARdelta DNA binding domain expressed in HEK293 cells by luciferase reporter gene assay Agonist activity at Gal4-fused human PPARdelta DNA binding domain expressed in HEK293 cells by luciferase reporter gene assay	[PMID: 21094606]
HEK293	EC₅₀	0.18 nM Compound: GW501516	Agonist activity at human PPARbeta expressed in HEK293 cells by luciferase reporter gene assay Agonist activity at human PPARbeta expressed in HEK293 cells by luciferase reporter gene assay	[PMID: 25305688]
HEK293	EC₅₀	0.0059 μM Compound: GW501516	Agonist activity at GAL4-tagged human PPARdelta ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay Agonist activity at GAL4-tagged human PPARdelta ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 27591006]
HEK293	EC₅₀	0.0059 μM Compound: GW501516	Agonist activity at N-terminal Gal4 fused human PPARdelta LBD transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay Agonist activity at N-terminal Gal4 fused human PPARdelta LBD transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 27622746]
HEK293	EC₅₀	0.0044 μM Compound: GW501516	Agonist activity at GAL4N fused human PPARdelta LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay Agonist activity at GAL4N fused human PPARdelta LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay	[PMID: 28539218]
HeLa	EC₅₀	>10000 nM Compound: 27, GW-501516	Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay	[PMID: 19275963]
HeLa	EC₅₀	8 nM Compound: 27, GW-501516	Agonist activity at PPARdelta ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay Agonist activity at PPARdelta ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay	[PMID: 19275963]
HeLa	EC₅₀	>10000 nM Compound: 27, GW-501516	Agonist activity at PPARalpha ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay Agonist activity at PPARalpha ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay	[PMID: 19275963]
HepG2	EC₅₀	4 nM Compound: GW-501516	Agonist activity at human PPARdelta in HepG2 cells by GAL4-luciferase reporter gene assay Agonist activity at human PPARdelta in HepG2 cells by GAL4-luciferase reporter gene assay	[PMID: 17512197]
HepG2	EC₅₀	0.0012 μM Compound: GW-501516	Agonist activity at human PPARdelta expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay Agonist activity at human PPARdelta expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay	[PMID: 21215640]
HepG2	EC₅₀	0.8 μM Compound: GW-501516	Agonist activity at human PPARgamma expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay Agonist activity at human PPARgamma expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay	[PMID: 21215640]
HepG2	EC₅₀	1.1 μM Compound: GW-501516	Agonist activity at human PPARalpha expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay Agonist activity at human PPARalpha expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay	[PMID: 21215640]
L6	EC₅₀	6 nM Compound: GW-501516	Effect on fatty acid oxidation in rat L6 cells Effect on fatty acid oxidation in rat L6 cells	[PMID: 17343371]

In Vitro

GW 501516 is shown to be the most potent and selective PPARδ agonists known with an EC₅₀ of 1.1 nM against PPARδ and 1000-fold selectivity over the other human subtypes, PPARα and-γ^[1].
GW 501516 exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells. GW 501516 inhibits palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner^[3].

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

In Vivo

GW 501516 causes impaired bone formation, leading to decreased BMD and deterioration of bone properties in OVX rats^[2].
GW 501516 attenuates interstitial inflammation and proximal tubular cell damage in a protein-overload mouse nephropathy model^[3].
GW 501516 treatment enhances running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice^[4].

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

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 317318-70-0
Appearance Solid
Masse moléculaire 453.50
Formule C₂₁H₁₈F₃NO₃S₂
Color White to off-white
SMILES

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

GW 1516; GSK-516
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (29)

All Cell Imaging/StainingWBCell Proliferation/Viability AssayIFCell Migration/Invasion Assay

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Journal Impact Factor

Nat Metab

Cellular Feimin enhances exercise performance by suppressing muscle thermogenesis. [Abstract]

2025 Jan;7(1):84-101. PMID: 39747484
Cell Stem Cell

Hepatic cytochrome P450 8B1 and cholic acid potentiate intestinal epithelial injury in colitis by suppressing intestinal stem cell renewal. [Abstract]

2022 Sep 1;29(9):1366-1381.e9. PMID: 36055192

GW 501516 purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2022 Sep 1;29(9):1366-1381.e9. [Abstract]

Crypts isolated from Lgr5-EGFP-IRES-creERT2 mice were cultured with CA together with/without 100 μM WY14643/ 10 μM Pioglitazone/ 1 μM GW501516 for 6 days. Representative staining pattern of Lgr5⁺ cells.
Cell Stem Cell

Epiblast inducers capture mouse trophectoderm stem cells in vitro and pattern blastoids for implantation in utero. [Abstract]

2022 Jul 7;29(7):1102-1118.e8. PMID: 35803228
J Adv Res

Endogenous hydrogen sulfide improves vascular remodeling through PPARδ/SOCS3 signaling. [Abstract]

2020 Jun 20;27:115-125. PMID: 33318871
Adv Sci (Weinh)

Erucic Acid, Derived by Lactobacillus Crispatus, Induces Ferroptosis in Cervical Cancer Organoids Through the PPAR-δ Signaling Pathway. [Abstract]

2025 Oct 13:e12599. PMID: 41082335

GW 501516 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Oct 13:e12599. [Abstract]

ROS assays of Ca Ski cells treated with DMSO, GW501516 (a PPARδ receptor agonists), Metformin (a promoter of fatty acid oxidation), EA, EA+DMSO, EA+GSK3787 (GSK3787 is a PPARδ receptor antagonist), EA+Fer‐1, CFS and CFS+ GSK3787. Blue fluorescence: Hoechst (nuclei of all the cells). Green fluorescence: ROS. Scale bars, 500 µm. B) Bar chart of the Acetyl‐CoA levels.

GW 501516 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Oct 13:e12599. [Abstract]

Edu assays of Ca Ski cells treated with 10%CFS, 10%CFS+GSK3787, 10%CFS+Fer‐1, GW501516, Metformin, EA and EA+ GSK3787. Blue fluorescence: Hoechst (nuclei of all the cells). Red fluorescence: 5‐Ethynyl‐2′‐deoxyuridine (proliferating cells).

GW 501516 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Oct 13:e12599. [Abstract]

Transwell assays of Ca Ski cells treated with 10%CFS, 10%CFS+GSK3787, 10%CFS+Fer‐1, GW501516, Metformin, EA and EA+ GSK3787. Scale bars, 100 µm.
Engineering

2024 Sep 6.
Cancer Lett

Activation of PPARδ in bone marrow endothelial progenitor cells improves their hematopoiesis-supporting ability after myelosuppressive injury. [Abstract]

2024 Jun 28:592:216937. PMID: 38704134
Phytomedicine

2025 Dec 28.
Int J Surg

Single-cell transcriptomics uncovers malignant potential of gallbladder adenomyomatosis and identifies PRDX1+ immunosuppressive macrophages in gallbladder carcinoma. [Abstract]

2026 Jan 23. PMID: 41570280
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
J Med Chem

Design, Synthesis, and Biological Evaluation of Arylimidazole Derivatives as Potent PPARδ Agonists for the Treatment of Renal Fibrosis. [Abstract]

2026 Feb 26;69(4):4469-4492. PMID: 41667192
J Med Chem

Design, Synthesis, and Biological Evaluation of Triazolone Derivatives as Potent PPARα/δ Dual Agonists for the Treatment of Nonalcoholic Steatohepatitis. [Abstract]

2022 Feb 10;65(3):2571-2592. PMID: 35060744
JCI Insight

Postprandial exercise regulates tissue-specific triglyceride uptake through angiopoietin-like proteins. [Abstract]

2024 Aug 22;9(16):e181553. PMID: 39171527
Eur J Med Chem

Design, synthesis and anti-diabetic evaluation of novel PPAR agonists based on functional group-oriented strategy. [Abstract]

2025 Oct 9:301:118226. PMID: 41075607
Eur J Med Chem

Design, synthesis, and biological evaluation of imidazolidinone derivatives as potent PPARα/δ agonists for the treatment of cholestatic liver diseases. [Abstract]

2025 Mar 15:286:117284. PMID: 39827490
Eur J Med Chem

Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis. [Abstract]

2024 Apr 5:269:116344. PMID: 38522113
J Chem Inf Model

Discovery of Novel Peroxisome Proliferator-Activated Receptor α (PPARα) Agonists by Virtual Screening and Biological Evaluation. [Abstract]

2020 Mar 23;60(3):1717-1727. PMID: 32027126
Mar Drugs

Novel PPAR-γ Agonist from the Soft Coral Sarcophyton crassocaule: Modulating Glucose Uptake and Lipid Droplet Formation. [Abstract]

2025 Nov 24;23(12):450. PMID: 41440884
Eur J Pharmacol

GW501516 facilitated tumor immune escape by inhibiting phagocytosis. [Abstract]

2025 Feb 22:177418. PMID: 39993702
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

GW 501516 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jun 28:9:648. [Abstract]

Western blot analysis of the protein expression of caspase and Bcl-2 family members in response to GW501516.
Molecules

Synthesis of Novel Farnesoid X Receptor Agonists and Validation of Their Efficacy in Activating Differentiation of Mouse Bone Marrow-Derived Mesenchymal Stem Cells into Osteoblasts. [Abstract]

2019 Nov 16;24(22):4155. PMID: 31744088
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
J Pharm Biomed Anal

Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]

2021 Feb 20:195:113870. PMID: 33453569
Am J Med Genet A

KRT6A Variant Underlies Pachyonychia Congenita: Insights Into Protein Aggregation and PPAR Signaling. [Abstract]

2026 Feb 26. PMID: 41744052
Elife

Exploration of precision coregulator TR-FRET identifies diverse signatures for LXR ligands relevant to discovery of nonlipogenic ABCA1 inducers. [Abstract]

2026 Jun 22:14:RP109146. PMID: 42325211
Biomed Pharmacother

Neonatal sevoflurane exposure disrupted fatty acids metabolism, leading to hypomyelination and neurological impairments. [Abstract]

2025 Oct:191:118495. PMID: 40925233
bioRxiv

2025 Oct 22.
SSRN

2025 Apr 27.
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

Solvant et solubilité

In Vitro:

DMSO : ≥ 100 mg/mL (220.51 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

2.2051 mL

11.0254 mL

22.0507 mL

5 mM

0.4410 mL

2.2051 mL

4.4101 mL

10 mM

0.2205 mL

1.1025 mL

2.2051 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, 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 (5.51 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.51 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (5.51 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)
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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 + +
%
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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

Protocole

Cell Assay^[3]

GW 501516 is dissolved in DMSO. Cells are starved by incubation in 0.2% FCS DMEM for 9 h, then pre-incubated with GW 501516, at a final concentration of 2.5 and 5 µM, or 0.05% DMSO as control for 3 hours, followed by stimulation with 150 µM palmitate bound to 8.0% BSA for 12 h^[3].

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

Animal Administration^[2]^[3]

Rats: Female Sprague Dawley rats, 12 weeks of age, are allocated to a sham-operated group and 3 OVX groups; high-dose GW 501516 (OVX-GW5), low-dose GW 501516 (OVX-GW1), and a control group (OVX-CTR), respectively. Animals receive GW 501516 or vehicle (methylcellulose) daily for 4 months by gavage. Bone mineral density (BMD) is assessed by dual x-ray absorptiometry at the femur, spine, and whole body^[2].

Mice: Mice are randomly allocated to different groups and receive therapeutic diet and treatment. The GW 501516-containing rodent diet is made by evenly adding GW 501516 to the control diet to a final concentration of 0.04% w/w. In the control diet, 10% of the total calories are from fat (5.5% from soybean oil and 4.5% from lard)^[3].

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
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- Portuguese - PT (254 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)
Instruction de manipulation (2659 KB)

Références

[1]. Wei ZL, et al. A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor delta. J Org Chem. 2003 Nov 14;68(23):9116-8. [Content Brief]

[2]. Mosti MP, et al. Effects of the peroxisome proliferator-activated receptor (PPAR)-δ agonist GW 501516 on bone and muscle in ovariectomized rats. Endocrinology. 2014 Jun;155(6):2178-89. [Content Brief]

[3]. Yang X, et al. GW 501516, a PPARδ agonist, ameliorates tubulointerstitial inflammation in proteinuric kidney disease via inhibition of TAK1-NFκB pathway in mice. PLoS One. 2011;6(9):e25271. [Content Brief]

[4]. Chen W, et al. A metabolomic study of the PPARδ agonist GW 501516 for enhancing running endurance in Kunming mice. Sci Rep. 2015 May 6;5:9884. [Content Brief]

[5]. Ji Y, et al. PPARβ/δ Agonist GW501516 Inhibits Tumorigenicity of Undifferentiated Nasopharyngeal Carcinoma in C666-1 Cells by Promoting Apoptosis. Front Pharmacol. 2018 Jun 28;9:648. [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, 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	2.2051 mL	11.0254 mL	22.0507 mL	55.1268 mL
	5 mM	0.4410 mL	2.2051 mL	4.4101 mL	11.0254 mL
	10 mM	0.2205 mL	1.1025 mL	2.2051 mL	5.5127 mL
	15 mM	0.1470 mL	0.7350 mL	1.4700 mL	3.6751 mL
	20 mM	0.1103 mL	0.5513 mL	1.1025 mL	2.7563 mL
	25 mM	0.0882 mL	0.4410 mL	0.8820 mL	2.2051 mL
	30 mM	0.0735 mL	0.3675 mL	0.7350 mL	1.8376 mL
	40 mM	0.0551 mL	0.2756 mL	0.5513 mL	1.3782 mL
	50 mM	0.0441 mL	0.2205 mL	0.4410 mL	1.1025 mL
	60 mM	0.0368 mL	0.1838 mL	0.3675 mL	0.9188 mL
	80 mM	0.0276 mL	0.1378 mL	0.2756 mL	0.6891 mL
	100 mM	0.0221 mL	0.1103 mL	0.2205 mL	0.5513 mL

Keywords

GW 501516

29 Cited Publications

100 mg Obtenir un devis

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GW 501516

Anti-diabetic Compound Library

Orally Active Compound Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Human Metabolite Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Mitochondrial Protection Compound Library

Metabolic Enzyme Compound Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) GW 501516

Voir tous les produits spécifiques à Isoform PPAR

Activité biologique

Chemical Information

Publications (29)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

GW 501516

Anti-diabetic Compound Library

Orally Active Compound Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Human Metabolite Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Mitochondrial Protection Compound Library

Metabolic Enzyme Compound Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) GW 501516

Voir tous les produits spécifiques à Isoform PPAR

Activité biologique

Chemical Information

Publications (29)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

GW 501516 Related Classifications

HY-10838 Related Classifications