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GW9662

GW9662是一种选择性PPAR拮抗剂,作用于PPARγ,无细胞试验中IC50为3.3 nM,在细胞中作用于PPARγ比作用于PPARα和PPARδ的功能选择性强10到600倍。

  • 货号:
    TK0283
  • 规格:
    1mg
    5mg
    10mg
    25mg
  • 价格:
    0.00

产品参数

CAS No.22978-25-2
生物活性GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.
分子式C13H9ClN2O3
分子量276.68
储存条件Powder -20℃ 3 years
溶解性数据DMSO : ≥ 100 mg/mL (361.43 mM) H2O : < 0.1 mg/mL (insoluble)
体内研究Bone marrow (BM) nucleated cell counts in both BADGE- and GW9662(1 mg/kg, i.p.)-treated mice are significantly higher than counts in the aplastic anemia (AA) group. GW9662 (1 mg/kg, i.p.) largely attenuates the renoprotective effects of Lipopolysaccharide (LPS) in the rat.
体外研究GW9662 inhibits radioligand binding to PPARγ, PPARα, and PPARδ with pIC50s of 8.48±0.27 (IC50=3.3 nM; n=10), 7.49±0.17 (IC50=32 nM; n=9), and 5.69±0.17 (IC50=2000 nM; n=3), respectively. GW9662 has nanomolar IC50 versus PPARγ and is 10- and 600-fold less potent in binding experiments using PPARα and PPARδ, respectively. In cell-based reporter assays, GW9662 is a potent and selective antagonist of full-length PPARγ. Co-treatment with both 50 μM BRL 49653 and 10 μM GW9662 results in statistically lower viable cell numbers after 7 days when compared to treatment with either 50 μM BRL 49653 (P=0.001) or 10 μM GW9662 (P=0.01) alone.
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纯度及产品资料98%