GW501516

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GW501516 ("GW1516") Chemical information IUPAC Nomenclature 2-(2-methyl-4-((4-methyl-2-(4-(trifluoromethyl)phenyl)thiazol-5-yl)methylthio)phenoxy)acetic acid Chemical Formula C21H18F3NO3S2 Molecular Weight 453.50 g/mol Clinical information Clinical Usage Exercise mimetic[1] Mechanism of Action PPARδ activator[2] Route of Administration Oral[1]
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GW501516, colloquially referred to as GW1516, IUPAC name 2-(2-methyl-4-((4-methyl-2-(4-(trifluoromethyl)phenyl)thiazol-5-yl)methylthio)phenoxy)acetic acid, is a small-molecule chemical compound that is a specific activator for the orphan nuclear receptor peroxisome proliferator-activated receptor (PPARδ).^[2]

It was characterized by Snzaidman et. al in 2003 at GlaxoSmithKline by a collaboration between research teams at North Carolina, United States of America and Les Ulis Cedex, France.

In 2008, Narkar et. al at the Salk Institute and the Howard Hughes Medical Institute at La Jolla, California would demonstrate that oral administration of 5mg/kg GW501516 to eight-week-old male C57B/6J mice mediates metabolic reprogramming of muscle to type I fast-twitch oxidative fibers, increasing fiber proportion by 38% and increasing mitochondrial DNA content by 50% in combination with compound administration and exercise.^[1]

[edit] References

1. ↑ ^{1.0 1.1 1.2} Narkar et. al (2008). AMPK and PPARδ Agonists Are Exercise Mimetics. Cell (134), 405–415.
2. ↑ ^{2.0 2.1} Sznaidman et. al (2003). Novel Selective Small Molecule Agonists for Peroxisome Proliferator-Activated Receptor δ (PPARδ)—Synthesis and Biological Activity. Bioorganic and Medicinal Chemistry Letters (13): 1517–1521.

Chemical Biology: Small-Molecule Control of Biological Systems (RelentlessRecusant)
Biological Targets		Compound Names
Receptor Tyrosine Kinases		A-83-01 (TGFβ/Activin) · BPIQ-II (EGFR) · Dorsomorphin/LDN-193189 (TGFβ/BMP) · SU5402 (FGFR)
Signaling Kinases		A-769662 (AMPK) · BMS-354825 (BCR-ABL, Src)· BIO-Acetoxime (GSK3) · CHIR99021 (GSK3) · GO 6976 (PKC) · IMD-0354 (IκBa) · PD184352 (MAPK) · SB203580 (MAPK) · Y-27632 (ROCK)
G Protein-Coupled Receptor		(+)-WIN-55212 (CB1/CB2) · ±-Sulpride (D2) · A 841720 (mGluR1) · BP-554 (5-HT1A) · Hh-Ag1.5 (Smo) · Cyclopamine/KAAD-Cyclopamine (Smo) · SANT1 (Smo) · SB-277011 (D3)
Ion Channels		BAY K8644 (Cav1.2) · Bicuculline (GABAAR) · Cymarin (Na+/H+) · G-strophanthin (Na+/H+) · L-AP4 (Na+/H+) · Oxcarbazepine (Na+) · Resiniferatoxin (TRPV1) · Sarmentogenin (Na+/H+) · Theanine (AMPAR, NMDAR)
Transporters		O-1783 (DAT) · WF-23 (DAT, SERT)
Nuclear Receptor		All-trans retinoic acid (RAR/RXR) · GW501516 (PPARδ) · RU-486 (Nr3c1, Nr3c3)
Protein Phosphatases		Endothall (PP2A)
Polypharmacological		Phosphoserine (mGluR4) · PK115-584 (Tcf4/β-catenin, PKC) · Pluripotin · Reversine
Other		2C-E (DAT) · 4-methoxyphenyl-HTI-286 (α/β-tubulin) · Compound E/DAPT (presenilin-1) · D-cysteine · D-phenylalanine · Flurbiprofen (COX) · JZL184 (MAGL) · QS11 (RAFGAP1) · RO-28-1675 (glucokinase) · Robotnikinin (Shh) · Selegiline (MAOB)
Uncharacterized		Neuropathiazol
Libraries		Kinase Inhibitor Library
Publications
Small molecule-mediated manipulation of the adult human induces selective and reversible control of physiological and psychological phenotype (Rubin et. al, 2590. Nature Medicine)
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