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MF63 is a selective mPGES-1 inhibitor (IC50: 0.9 nM and 1.3 nM for pig mPGES-1 and human mPGES-1 enzyme, respectively).
Description | MF63 is a selective mPGES-1 inhibitor (IC50: 0.9 nM and 1.3 nM for pig mPGES-1 and human mPGES-1 enzyme, respectively). |
In vitro | MF63 strongly inhibited guinea pig mPGES-1 but not the mouse or rat enzyme, in rodent species. mPGES-1 MF63 potently inhibited the human mPGES-1 enzyme with a high degree (>1000-fold) of selectivity over other prostanoid synthases. The compound selectively inhibited the synthesis of PGE(2) when tested in the guinea pig and a knock-in (KI) mouse expressing human mPGES-1, but not other prostaglandins inhibitable by nonsteroidal anti-inflammatory drugs (NSAIDs), yet retained NSAID-like efficacy at inhibiting lipopolysaccharide-induced pyresis, hyperalgesia, and iodoacetate-induced osteoarthritic pain. |
Molecular Weight | 378.81 |
Formula | C23H11ClN4 |
Cas No. | 892549-43-8 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 43 mg/mL (113.51 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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