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An AAK1 inhibitor that reduces phosphorylation of AP2M2 in HEK293 cells overexpressing AAK1 and AP2M2 (IC50 = 0.051 µM), selective for AAK1 over a panel of 219 kinases, including BIKE, GAK, and STK16 (IC550 = 0.120, 1.06, and 15.8 µM, respectively), inhibits AP2M2 phosphorylation in mouse brain lysates (ED50 = 6 mg/kg), reduces formalin-induced paw flinch and biting in a rat model of persistent pain at 30 mg/kg, reduces thermal and mechanical hyperalgesia, as well as cold and mechanical allodynia, in a rat model chronic constriction injury at 60 mg/kg. SMILES: FC(F)OC1=C(C2=CN=CO2)C=CC(NC([C@H](N)CC(C)C)=O)=C1. InChi Code: InChI=1S/C16H19F2N3O3/c1-9(2)5-12(19)15(22)21-10-3-4-11(14-7-20-8-23-14)13(6-10)24-16(17)18/h3-4,6-9,12,16H,5,19H2,1-2H3,(H,21,22)/t12-/m1/s1. InChi Key: GCTFTMWXZFLTRR-GFCCVEGCSA-N
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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