GW501516 is a specific agonist for PPARδ (EC50=1.1nM) with a 1'000-fold selectivity over the other human subtypes.
Product Details
| Formula: | C21H18F3NO3S2 |
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| MW: | 453.5 |
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| CAS: | 317318-70-0 |
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| Purity: | ≥98% (HPLC) |
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| Identity: | Identity determined by 1H-NMR and 13C-NMR. |
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| Appearance: | White to off-white solid. |
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| Solubility: | Soluble in DMSO (50mg/ml), dimethyl formamide (25mg/ml), 100% ethanol (12mg/ml) or methanol (50mg/ml); slightly soluble in water. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | +4°C |
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| Handling: | Protect from light. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
PPARγ inhibits small airway remodeling through mediating the polarization homeostasis of alveolar macrophages in COPD: S. He, et al.; Clin. Immunol.
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Acetyl-CoA-Carboxylase 1-mediated de novo fatty acid synthesis sustains Lgr5+ intestinal stem cell function: S. Li, et al.; Nat. Commun.
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Abstract;
PPARδ Inhibits Hyperglycemia-Triggered Senescence of Retinal Pigment Epithelial Cells by Upregulating SIRT1: E.J. Lee, et al.; Antioxidants
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Abstract;
Peroxisome proliferator-activated receptor δ rescues xCT-deficient cells from ferroptosis by targeting peroxisomes: J.S. Hwang, et al.; Biomed. Pharmacother.
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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.
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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;
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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;
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Ligand-activated PPARδ inhibits angiotensin II-stimulated hypertrophy of vascular smooth muscle cells by targeting ROS: E.S. Kang, et al.; PLoS One
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Abstract;
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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),
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CRY1/2 Selectively Repress PPARd and Limit Exercise Capacity: S.D. Jordan, et al.; Cell Metab.
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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.
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Abstract;
PPARβ/δ ameliorates fructose-induced insulin resistance in adipocytes by preventing Nrf2 activation: E. Barroso, et al.; Biochim. Biophys. Acta
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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),
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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
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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.
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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;
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;
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;
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;
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),
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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.
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Peroxisome-proliferator-activated receptor delta activates fat metabolism to prevent obesity: Y.X. Wang, et al.; Cell
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PPARdelta activation induces COX-2 gene expression and cell proliferation in human hepatocellular carcinoma cells: B. Glinghammar, et al.; BBRC
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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.
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Abstract;
A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport: W.R. Oliver, Jr., et al.; PNAS
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Abstract;
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