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S80635

GW0742

源叶(MedMol) 98%
  • 英文名:
  • GW0742
  • 别名:
  • Acetic acid, 2-[4-[[[2-[3-fluoro-4-(trifluoromethyl)phenyl]-4-methyl-5-thiazolyl]methyl]thio]-2-methylphenoxy]-
  • CAS号:
  • 317318-84-6
  • 分子式:
  • C21H17F4NO3S2
  • 分子量:
  • 471.49
  • MDL:
  • MFCD07369423
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S80635-1mg 98% ¥262.00元 10 - - - EA 加入购物车
源叶(MedMol) S80635-5mg 98% ¥600.00元 10 - - - EA 加入购物车
源叶(MedMol) S80635-10mg 98% ¥950.00元 8 - - - EA 加入购物车
源叶(MedMol) S80635-25mg 98% ¥1710.00元 6 - - - EA 加入购物车
源叶(MedMol) S80635-50mg 98% ¥2950.00元 2 - - - EA 加入购物车
源叶(MedMol) S80635-100mg 98% ¥5200.00元 1 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: GW0742 is a potent PPARβ and PPARδ agonist, with an IC50 of 1 nM for human PPARδ in binding assay, and EC50s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ, respectively.
  • 靶点: PPARδ:1 nM (EC50);PPARα:1.1 μM (EC50);PPARγ:2 μM (EC50);PPAR
  • 体内研究:
    GW0742 (0.3 mg/kg, i.p.) reduces intensity masson-trichrome staining, and attenuates the histological signs in bleomycin instillatio (BLEO)-induced lung injury of mice. GW0742 (0.3 mg/kg, i.p.) also causes a reduction of the BLEO-induced loss body weight, and a decrease of myeloperoxidase (MPO) activity. GW0742 shows significant inhibition of TNF-a and IL-1β in instilled-mice. GW0742 prevents bleomycin-induced IkB-a degradation, reduces the levels of NF-kB p65 in the lung, and decreases iNOS and p-ERK expression in BLEO-induced mice. GW0742 (5 mg/kg/day, i.v.) increases PPARδ protein level in the heart of rats. GW0742 also induces the increase in LCAD, VLCAD, and ACOX1 in the heart of rats
  • 参考文献:
    1. Sznaidman ML, et al. Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity. Bioorg Med Chem Lett. 2003 May 5;13(9):1517-21. 2. Smith SA, et al. Effect of the peroxisome proliferator-activated receptor beta activator GW0742 in rat cultured cerebellar granule neurons. J Neurosci Res. 2004 Jul 15;77(2):240-9. 3. Galuppo M, et al. GW0742, a high affinity PPAR-β/δ agonist reduces lung inflammation induced by bleomycin instillation in mice. Int J Immunopathol Pharmacol. 2010 Oct-Dec;23(4):1033-46. 4. Kuo SC, et al. Activation of receptors δ (PPARδ) by agonist (GW0742) may enhance lipid metabolism in heart both in vivo and in vitro. Horm Metab Res. 2013 Nov;45(12):880-6.
  • 溶解性: Soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.121 ml 10.605 ml 21.209 ml
    5 mM 0.424 ml 2.121 ml 4.242 ml
    10 mM 0.212 ml 1.06 ml 2.121 ml
    50 mM 0.042 ml 0.212 ml 0.424 ml
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