SAfit2 Chemical Properties

Boiling point:

877.0±65.0 °C(Predicted)

Density 

1.168±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMF: 50 mg/ml; DMSO: 50 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: 10 mg/ml

form 

A crystalline solid

pka

6.43±0.10(Predicted)

color 

Off-white to pink

SAfit2 Usage And Synthesis

Description

SAfit2 is a potent inhibitor of FK506-binding protein 51 (FKBP51; K_i = 6 nM). 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.

Uses

SAFit2 is a highly selective inhibitor of FKBP51. The selective inhibition of FKBP51, using SAFit1(S139583) & SAFit2 , has shown to enhances neurite elongation in neuronal cultures and improves neuroendocrine feedback and stress-coping behavior in mice.