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本试剂(2-(4-((2-(4-(三氟甲基)苯基)-5-甲基噻唑-4-基)甲基硫基)-2-甲基苯氧基)乙酸)
仅供科研实验使用,不得用于其他用途！
简介：
货 号：LC1-G-4789
名 称：2-(4-((2-(4-(三氟甲基)苯基)-5-甲基噻唑-4-基)甲基硫基)-2-甲基苯氧基)乙酸
别 名：GW501516 Free Acid
C A S ：317318-70-0
分子量：453.5
分子式：C21H18F3NO3S2
纯 度：HPLC/TLC:>99%
说 明：Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO. Disposal: A.
文 献：In vitro, GW501516 increased expression of the reverse cholesterol transporter ATP-binding cassette A1 and induced apolipoprotein A1-specific cholesterol efflux. In vivo, GW501516 dramatically increased serum high density lipoprotein cholesterol while lowering the levels of small-dense low density lipoprotein, fasting triglycerides, and fasting insulin when dosed to insulin-resistant middle-aged obese rhesus monkeys. Oliver, W.R. Jr., et al. "A selective peroxisome proliferator-activated receptor δ agonist promotes reverse cholesterol transport." Proc. Natl. Acad. Sci. USA 98: 5306-5311 (2001).Treatment of skeletal muscle cells by GW501516 resulted in the expression of genes involved in lipid utilization, β-oxidation, cholesterol efflux, and energy uncoupling. Furthermore, the treatment also increased apolipoprotein-A1 specific efflux of intracellular cholesterol, indicating the muscle tissue is an important target of PPARβ/δ agonists. Dressel, U., et al. "The peroxisome proliferator-activated receptor β/δ agonist, GW501516, regulates the expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells." Mol. Endocrinol. 17: 2477-2493 (2003).GW501516 induced fatty acid β-oxidation in L6 myotubes and in mouse skeletal muscles. GW501516 treatment to mice fed a high-fat diet ameliorated diet-induced obesity as well as insulin resistance. GW501516 treatment also dramatically improved diabetes, as demonstrated by the decrease in plasma glucose and blood insulin levels in genetically obese ob/ob mice. Tanaka, T., et al. "Activation of peroxisome proliferator-activated receptor δ induces fatty acid β-oxidation in skeletal muscle and attenuates metabolic syndrome." Proc. Natl. Acad. Sci. USA 100: 15924-15929 (2003).GW501516 protected against cytotoxin-induced SH-SY5Y cell injury in vitro. It also significantly attenuated the ischemic brain damage and MPTP-induced depletion of striatal dopamine and related metabolite contents in mouse brain. Iwashita, A., et al. "Neuroprotective efficacy of the peroxisome proliferator-activated receptor δ-selective agonists in vitro and in vivo." J. Pharmacol. Exp. Ther. 320: 1087-1096 (2007).GW501516 treatment did not stimulate the growth of human cancer cell lines including HT29, HCT116, LS-174T, HepG2, and HuH7. Hollingshead, H.E., et al. "Peroxisome proliferator-activated receptor-β/δ (PPARβ/δ) ligands do not potentiate growth of human cancer cell lines." Carcinogenesis 28: 2641-2649 (2007).GW501516 was identified as an orally active agent that would mimic or potentiate the effects of exercise. Narkar, V.A., et al. "AMPK and PPARδ agonists are exercise mimetics." Cell 134: 405-415 (2008).GW 501516 reduced the IFNγ-induced up-regulation of TNFα and inducible NO synthase, and showed anti-inflammatory activity. Defaux, A., et al. "Effects of the PPAR-β agonist GW501516 in an in vitro model of brain inflammation and antibody-induced demyelination." J. Neuroinflammation 6: 15 (2009).
