A potent

MF63 – 1 mg

Brand:
Cayman
CAS:
892549-43-8
Storage:
22
UN-No:
Non-Hazardous - /

Microsomal prostaglandin E2 synthase-1 (mPGES-1) is the terminal enzyme in the biosynthesis of PGE2.{19887,16438,18830} MF63 is a potent, selective, and orally active inhibitor of human mPGES-1 (IC50 = 1.3 nM).{27593,27594} It displays greater than 1,000-fold selectivity over other prostanoid synthases.{27594} MF63 also potently inhibits guinea pig mPGES-1 (IC50 = 0.9 nM) but not mouse or rat mPGES-1.{27594} In guinea pigs or in mice expressing human mPGES-1, MF63 prevents LPS-induced pyresis, hyperalgesia, and iodoacetate-induced osteoarthritic pain.{27594} It does not produce the gastrointestinal toxicity that is caused by non-selective COX inhibitors, although it markedly suppresses PGE2 synthesis in the stomach.{27594}  

 

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Description

A potent, selective, and orally active inhibitor of human mPGES-1 (IC50 = 1.3 nM); potently inhibits guinea pig mPGES-1 (IC50 = 0.9 nM) but not mouse or rat mPGES-1; prevents LPS-induced pyresis, hyperalgesia, and iodoacetate-induced osteoarthritic pain

Formal name: 2-(9-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-1,3-benzenedicarbonitrile

Synonyms: 

Molecular weight: 378.8

CAS: 892549-43-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Prostaglandin Synthases||Research Area|Immunology & Inflammation|Arthritis (Non-autoimmune)||Research Area|Immunology & Inflammation|Inflammatory Lipid Mediators|Prostaglandins||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway

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