CAY10678

CAY10678

CAT N°: 15129
Price:

From 92.00 78.20

Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 into the biologically active PGE2.{7229} Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1?, and TNF-?.{11537} CAY10678 is a benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC50 = 0.09 and 0.9 µM, respectively).{23940} It has minimal effects on COX-1, COX-2, PGIS, and hematopoietic PGDS at 50 ?M but reduces lipocalin-type PGDS activity by 60% at this concentration.{23940} CAY10678 dose-dependently blocks PGE2 synthesis in isolated cells and whole blood treated with LPS or IL-1?.{23940} It also dose-dependently reduces PGE2 synthesis and cell recruitment during inflammation in mice.{23940}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • N-cyclopentyl-1-[5,6-dimethyl-1-(1-methylethyl)-1H-benzimidazol-2-yl]-4-piperidinecarboxamide
  • Correlated keywords
    • inhibitors cyclooxygenases inflammation pains COXs inhibits inhibitions prostaglandins PGs PGES mPGES CAYs 10678 CAY-10678 benzoimidazole synthesis microsomal synthase hematopoietic lipocalin potent mPGES1 mPGES-1 1 one E synthase-1 PGH2 PGH 2 two PGE2 COX-2 induced pro-inflammatory proinflammatory pro inflammatory mediators LPS IL-1.beta. IL-1beta IL-1B IL-1? ? IL beta .beta. interleukins TNF-? TNF-alpha TNF-.alpha. alpha .alpha. ? TNFs humans rats recombinant COX-1 PGIS PGDS lipocalin-type dose-dependent doses dependents blocks cells blood recruitment mice
  • Product Overview:
    Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 into the biologically active PGE2.{7229} Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1?, and TNF-?.{11537} CAY10678 is a benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC50 = 0.09 and 0.9 µM, respectively).{23940} It has minimal effects on COX-1, COX-2, PGIS, and hematopoietic PGDS at 50 ?M but reduces lipocalin-type PGDS activity by 60% at this concentration.{23940} CAY10678 dose-dependently blocks PGE2 synthesis in isolated cells and whole blood treated with LPS or IL-1?.{23940} It also dose-dependently reduces PGE2 synthesis and cell recruitment during inflammation in mice.{23940}

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