产品描述:
PF-3084014 is a γ-secretase inhibitor (IC50s = 6.2 and 1.2 nM in an enzyme assay and in whole cells, respectively).{45150} It inhibits γ-secretase activity without inducing Notch-related toxicity (EC50s = 1,300-3,000 nM for B cells in fetal thymic organ cultures). It reduces the level of amyloid-β (1-40) (Aβ40) fragments in mouse brain three hours following administration of 1 to 18 mg/kg doses and reduces Aβ42 fragment levels when administered at doses of 9 or 18 mg/kg. It also reduces Aβ fragments in guinea pig brain when administered at doses ranging from 0.3 to 3 mg/kg per day for five days.