SAfit2

SAfit2 is a potent inhibitor of FK506-binding protein 51 (FKBP51; K_i = 6 nM).¹ It is highly selective for FKBP51 over FKBP52 (K_i = >50,000 nM) and has increased brain permeability in comparison to SAfit1. SAfit2 (20 mg/kg) enhances HPA axis suppression in mice by decreasing plasma corticosterone levels to a greater extent than in control mice following dexamethasone administration. It also does not increase plasma corticosterone levels as high as in control mice following subsequent administration of corticotropin-releasing factor (CRF). It decreases the time spent immobile in the forced swim test and increases the time spent in the open arms of the elevated plus maze, indicating antidepressant-like and anxiolytic-like activity, respectfully.²

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1. Gaali, S., Kirschner, A., Cuboni, S., et al. Selective inhibitors of the FK506-binding protein 51 by induced fit. Nat. Chem. Biol. 11(1), 33-37 (2015).

2. Hartmann, J., Wagner, K.V., Gaali, S., et al. Pharmacological inhibition of the psychiatric risk factor FKBP51 has anxiolytic properties. J. Neurosci. 35(24), 9007-9016 (2015).