| Identification | Back Directory | [Name]
SAfit2 | [CAS]
1643125-33-0 | [Synonyms]
SAfit2
2-Piperidinecarboxylic acid, 1-[(2S)-2-cyclohexyl-2-(3,4,5-trimethoxyphenyl)acetyl]-, (1R)-3-(3,4-dimethoxyphenyl)-1-[3-[2-(4-morpholinyl)ethoxy]phenyl]propyl ester, (2S)- | [Molecular Formula]
C46H62N2O10 | [MDL Number]
MFCD31619236 | [MOL File]
1643125-33-0.mol | [Molecular Weight]
802.99 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [Description]
SAfit2 is a potent inhibitor of FK506-binding protein 51 (FKBP51; Ki = 6 nM). It is highly selective for FKBP51 over FKBP52 (Ki = >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. |
|
|