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PPARδ agonist
GW501516 is a specific agonist for PPARδ (EC50=1.1nM) with a 1’000-fold selectivity over the other human subtypes.
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Product Details
| Appearance |
White to off-white solid. |
|---|---|
| CAS |
317318-70-0 |
| Couple Target |
PPAR |
| Couple Type |
Activator, Ligand |
| Formula |
C21H18F3NO3S2 |
| Identity |
Identity determined by 1H-NMR and 13C-NMR. |
| MW |
453.5 |
| Purity |
≥98% (HPLC) |
| Solubility |
Soluble in DMSO (50mg/ml), dimethyl formamide (25mg/ml), 100% ethanol (12mg/ml) or methanol (50mg/ml); slightly soluble in water. |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. |
|---|---|
| Handling |
Protect from light. |
| Long Term Storage |
+4°C |
| Shipping |
Ambient Temperature |
| Regulatory Status |
RUO – Research Use Only |
|---|
- PPARγ inhibits small airway remodeling through mediating the polarization homeostasis of alveolar macrophages in COPD: S. He, et al.; Clin. Immunol. 250, 109293 (2023), Abstract
- Acetyl-CoA-Carboxylase 1-mediated de novo fatty acid synthesis sustains Lgr5+ intestinal stem cell function: S. Li, et al.; Nat. Commun. 13, 3998 (2022), Abstract
- PPARδ Inhibits Hyperglycemia-Triggered Senescence of Retinal Pigment Epithelial Cells by Upregulating SIRT1: E.J. Lee, et al.; Antioxidants 11, 1207 (2022), Abstract
- Peroxisome Proliferator-Activated Receptor Activation in Precision-Cut Bovine Liver Slices Reveals Novel Putative PPAR Targets in Periparturient Dairy Cows: Busato, S., Ford, H. R., et al.; Front. Vet. Sci. 9, 931264 (2022), Abstract
- Peroxisome proliferator-activated receptor δ rescues xCT-deficient cells from ferroptosis by targeting peroxisomes: J.S. Hwang, et al.; Biomed. Pharmacother. 143, 112223 (2021), Abstract
- Peroxisome proliferator-activated receptor-δ-mediated upregulation of catalase helps to reduce ultraviolet B-induced cellular injury in dermal fibroblasts: J. Hur, et al.; J. Dermatol. Sci. 923, 170 (2021), Abstract
- Increase in muscle endurance in mice by dietary Yamabushitake mushroom (Hericium erinaceus) possibly via activation of PPARδ: Y. Komiya, et al.; Anim. Sci. J. 90, 781 (2019), Abstract — Full Text
- Cholesterol metabolism is a druggable axis that independently regulates tau and amyloid-β in iPSC-derived Alzheimer’s disease neurons: R. van der Kant, et al.; Cell Stem Cell 24, 363 (2019), Abstract — Full Text
- Ligand-activated PPARδ inhibits angiotensin II-stimulated hypertrophy of vascular smooth muscle cells by targeting ROS: E.S. Kang, et al.; PLoS One 14, e0210482 (2019), Abstract — Full Text
- Ligand-Activated Peroxisome Proliferator-Activated Receptor δ Attenuates Vascular Oxidative Stress by Inhibiting Thrombospondin-1 Expression: M.Y. Ahn, et al.; J. Vasc. Res. 55, 75 (2018), Abstract
- PPARδ Elicits Ligand-Independent Repression of Trefoil Factor Family to Limit Prostate Cancer Growth: Martín-Martín, N., Zabala-Letona, A., et al.; Cancer Res. 78, 399 (2018), Abstract
- CRY1/2 Selectively Repress PPARd and Limit Exercise Capacity: S.D. Jordan, et al.; Cell Metab. 26, 243 (2017), Abstract — Full Text
- Circadian repressors CRY1 and CRY2 broadly interact with nuclear receptors and modulate transcriptional activity: Kriebs, A., Jordan, S. D., et al.; PNAS 114, 8776 (2017), Abstract
- High-fat diet enhances stemness and tumorigenicity of intestinal progenitors: Beyaz, S., Mana, M. D., et al.; Nature 531, 53 (2016), Abstract
- Fungus-Derived Neoechinulin B as a Novel Antagonist of Liver X Receptor, Identified by Chemical Genetics Using a Hepatitis C Virus Cell Culture System: Nakajima, S., Watashi, K., et al.; J. Virol. 90, 9058 (2016), Abstract
- Tracing the molecular basis of transcriptional dynamics in noisy data by using an experiment-based mathematical model: Rybakova, K. N., Tomaszewska, A., et al.; Nucleic Acids Res. 43, 153 (2015), Abstract
- Ligand-activated PPARδ upregulates α-smooth muscle actin expression in human dermal fibroblasts: a potential role for PPARδ in wound healing: S.A. Ham, et al.; J. Dermatol. Sci. 80, 186 (2015), Application(s): Cell Culture, Abstract
- PPARβ/δ ameliorates fructose-induced insulin resistance in adipocytes by preventing Nrf2 activation: E. Barroso, et al.; Biochim. Biophys. Acta 1852, 1049 (2015), Application(s): Cell Culture, Abstract
- PPARδ modulates oxLDL-induced apoptosis of vascular smooth muscle cells through a TGF-β/FAK signaling axis: J.S. Hwang, et al.; Int. J. Biochem. Cell. Biol. 62, 54 (2015), Application(s): Cell Culture, Abstract
- Ligand-activated PPARδ modulates the migration and invasion of melanoma cells by regulating Snail expression: Ham, S. A., Yoo, T., et al.; Am. J. Cancer Res. 4, 674 (2014), Abstract
- Activation of the retinoid X receptor modulates angiotensin II-induced smooth muscle gene expression and inflammation in vascular smooth muscle cells: Lehman, A. M., Montford, J. R., et al.; Mol. Pharmacol. 86, 570 (2014), Abstract
- Activation of PPARδ prevents endothelial dysfunction induced by overexpression of amyloid-β precursor protein: d’Uscio, L. V., Das, P., et al.; Cardiovasc. Res. 96, 504 (2012), Abstract
- An ethanol extract of Artemisia iwayomogi activates PPARδ leading to activation of fatty acid oxidation in skeletal muscle: Cho, S. Y., Jeong, H. W., et al.; PLoS One 7, e33815 (2012), Abstract
- A PML–PPAR-δ pathway for fatty acid oxidation regulates hematopoietic stem cell maintenance: Ito, K., Carracedo, A., et al.; Nat. Med. 18, 1350 (2012), Abstract
- Development of a cell-based, high-throughput screening assay for cholesterol efflux using a fluorescent mimic of cholesterol: Zhang, J., Cai, S., et al.; Assay. Drug Dev. Technol. 9, 136 (2011), Abstract
- Activation of peroxisome proliferator-activated receptor-{delta} by GW501516 prevents fatty acid-induced nuclear factor-{kappa}B activation and insulin resistance in skeletal muscle cells: T. Coll, et al.; Endocrinology 151, 1560 (2010), Abstract
- Activation of PPARs α, β/δ, and γ Impairs TGF-β1-Induced Collagens’ Production and Modulates the TIMP-1/MMPs Balance in Three-Dimensional Cultured Chondrocytes: Poleni, P. E., Etienne, S., et al.; PPAR Res. 2010, 635912 (2010), Abstract
- Activation of PPARdelta promotes mitochondrial energy metabolism and decreases basal insulin secretion in palmitate-treated beta-cells: L. Jiang, et al.; Mol. Cell. Biol. 343, 249 (2010), Abstract
- PPARbeta activation inhibits melanoma cell proliferation involving repression of the Wilms’ tumour suppressor WT1: Michiels, J. F., Perrin, C., et al.; Pflugers Arch. 459, 689 (2010), Abstract
- Cross-talk between vitamin D receptor (VDR)- and peroxisome proliferator-activated receptor (PPAR)-signaling in melanoma cells: P. Sertznig, et al.; Anticancer Res. 29, 3647 (2009), Abstract
- Population-level transcription cycles derive from stochastic timing of single-cell transcription: Degenhardt, T., Rybakova, K. N., et al.; Cell 138, 489 (2009), Abstract
- Effects of the PPAR-beta agonist GW501516 in an in vitro model of brain inflammation and antibody-induced demyelination: A. Defaux, et al.; J. Neuroinflammation 6, 15 (2009), Abstract
- Pharmacological activation of PPARbeta/delta stimulates utrophin A expression in skeletal muscle fibers and restores sarcolemmal integrity in mature mdx mice: Miura, P., Chakkalakal, J. V., et al.; Hum. Mol. Genet. 18, 4640 (2009), Abstract
- Determination of the critical amino acids involved in the peroxisome proliferator-activated receptor (PPAR) delta selectivity of phenylpropanoic acid-derived agonists: J. Kasuga, et al.; Chem. Med. Chem. 3, 1662 (2008), Abstract
- PPARgamma regulates the function of human dendritic cells primarily by altering lipid metabolism: Szatmari, I., Töröcsik, D., et al.; Blood 110, 3271 (2007), Abstract
- Meta-analysis of primary target genes of peroxisome proliferator-activated receptors: Heinaniemi, M., Uski, J. O., et al.; Genome Biol. 8, R147 (2007), Abstract
- SLIRP, a small SRA binding protein, is a nuclear receptor corepressor: Hatchell, E. C., Colley, S. M., et al.; Mol. Cell 22, 657 (2006), Abstract
- The peroxisome proliferator-activated receptor beta/delta agonist, GW501516, regulates the expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells: U. Dressel, et al.; Mol. Endocrinol. 17, 2477 (2003), Abstract
- A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor delta: Z.L. Wei & A.P. Kozikowski; J. Org. Chem. 68, 9116 (2003), Abstract
- Peroxisome-proliferator-activated receptor delta activates fat metabolism to prevent obesity: Y.X. Wang, et al.; Cell 113, 159 (2003), Abstract
- PPARdelta activation induces COX-2 gene expression and cell proliferation in human hepatocellular carcinoma cells: B. Glinghammar, et al.; BBRC 308, 361 (2003), Abstract
- Peroxisome proliferator-activated receptor (PPAR) alpha and PPARbeta/delta, but not PPARgamma, modulate the expression of genes involved in cardiac lipid metabolism: A.J. Gilde, et al.; Circ. Res. 92, 518 (2003), Abstract
- Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)-synthesis and biological activity: M.L. Sznaidman, et al.; Bioorg. Med. Chem. Lett. 13, 1517 (2003), Abstract
- A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport: W.R. Oliver, Jr., et al.; PNAS 98, 5306 (2001), Abstract — Full Text
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