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It targets the enzyme active site and is primarily competitive with the substrate and noncompetitive toward the cofactor
surface plasmon resonance and 1H-15N transverse relaxation-optimized spectroscopy (TROSY) NMR spectroscopy
resulting in the impairment of cell growth
Chassande O
CAS Number: 2260791-14-6
PF-8380 03-204 It targets the enzyme activePF 8380 is a potent autotaxin inhibitor with an IC(50) of 2. 8 nM in isolated enzyme assay and 101 nM in human whole blood. PF 8380 has adequate oral bioavailability and exposures required for in vivo testing of autotaxin inhibition. Autotaxin's role in producing LPA in plasma and at the site of inflammation was tested in a rat air pouch model. The specific inhibitor PF 8380 , dosed orally at 30 mg kg, provided >95% reduction in both plasma and air
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