A benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC50 = 0.09 and 0.9 µM

CAY10678 – 1 mg

Brand:
Cayman
CAS:
1268709-57-4
Storage:
-20
UN-No:
Non-Hazardous - /

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-1β, and TNF-α.{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 μM 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-1β.{23940} It also dose-dependently reduces PGE2 synthesis and cell recruitment during inflammation in mice.{23940}  

 

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Description

A benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC50 = 0.09 and 0.9 µM, respectively); dose-dependently blocks PGE2 synthesis in isolated cells and whole blood treated with LPS or IL-1β; dose-dependently reduces PGE2 synthesis and cell recruitment during inflammation in mice

Formal name: N-cyclopentyl-1-[5,6-dimethyl-1-(1-methylethyl)-1H-benzimidazol-2-yl]-4-piperidinecarboxamide

Synonyms:  mPGES-1 Inhibitor III

Molecular weight: 382.5

CAS: 1268709-57-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Prostaglandin Synthases||Research Area|Immunology & Inflammation|Inflammatory Lipid Mediators|Prostaglandins||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway||Research Area|Neuroscience

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