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CAY10678

A mPGES-1 inhibitor

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CAY10678的二维码
  • 库存: 现货
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    促销价
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  • 1mg
    ¥1037.00
    830.00
    - +
  • 5mg
    ¥2825.00
    2260.00
    - +
  • 10mg
    ¥4025.00
    3220.00
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  • 货号: ajci22050
  • CAS: 1268709-57-4
  • 别名: mPGES-1 Inhibitor III
  • 分子式: C23H34N4O
  • 分子量: 382.5
  • 纯度: >98%
  • 溶解度: DMF: 15 mg/ml,DMSO: 5 mg/ml,Ethanol: 25 mg/ml,Ethanol:PBS (pH 7.2) (1:8): 0.1 mg/ml
  • 储存: Store at -20°C
  • 库存: 现货

Background

Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 into the biologically active PGE2. Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α. CAY10678 is a benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC50 = 0.09 and 0.9 uM, respectively). It has minimal effects on COX-1, COX-2, PGIS, and hematopoietic PGDS at 50 μM but reduces lipocalin-type PGDS activity by 60% at this concentration. CAY10678 dose-dependently blocks PGE2 synthesis in isolated cells and whole blood treated with LPS or IL-1β. It also dose-dependently reduces PGE2 synthesis and cell recruitment during inflammation in mice.

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