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CAS No. : 1360622-01-0
MCE 国际站:Vipoglanstat
产品活性:Vipoglanstat (BI 1029539),甲酰胺,是一种有效的,选择性的,非肽人前列腺素 E 合成酶 1 (mPGES-1) 小分子抑制剂,具有口服活性。Vipoglanstat 也具有抗炎活性。
研究领域:Immunology/Inflammation
作用靶点:PGE synthase
In Vitro: Vipoglanstat significantly inhibits mPGES-1 level (IC50: about 1 nM).
Vipoglanstat blocks the up-regulation of P-gp and mPGES-1 levels on glutamate-mediatedin isolated brain capillaries.
Vipoglanstat reduces human peripheral blood inflammatory cell migration and inflammatory mediator release.
In Vivo: Vipoglanstat (30 mg/kg; i.p.) can reduce LPS-induced lung injury, with reduction in neutrophil influx, protein content, TNF-ɑ, IL-1β and PGE2 levels in bronchoalveolar lavage (BAL), myeloperoxidase activity, expression of mPGES-1, cyclooxygenase (COX)-2 and intracellular adhesion molecule in lung tissue.
Vipoglanstat (30 mg/kg; p.o.; 2 h, 8 h and 22 h) significantly reduces sepsis-induced BAL inflammatory cell recruitment, lung injury score and lung expression of mPGES-1 and inducible nitric oxide synthase.
Vipoglanstat (30 mg/kg; p.o.; QD) also significantly prolongs survival of mice with severe sepsis.
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