SAfit2
SAfit2 Basic information
- Product Name:
- SAfit2
- 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)-
- (R)-3-(3,4-Dimethoxyphenyl)-1-(3-(2-morpholinoethoxy)phenyl)propyl (S)-1-((S)-2-cyclohexyl-2-(3,4,5-trimethoxyphenyl)acetyl)piperidine-2-carboxylate
- (1R)-3-(3,4-dimethoxyphenyl)-1-{3-[2-(morpholin-4-yl)ethoxy]phenyl}propyl (2S)-1-[(2S)-2-cyclohexyl-2-(3,4,5-trimethoxyphenyl)acetyl]piperidine-2-carboxylate
- SAFit2, 10 mM in DMSO
- CAS:
- 1643125-33-0
- MF:
- C46H62N2O10
- MW:
- 802.99
- Mol File:
- 1643125-33-0.mol
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
- InChIKey
- ZDBWLRLGUBSLPG-FDHYQTMZSA-N
- SMILES
- N1(C([C@@H](C2CCCCC2)C2=CC(OC)=C(OC)C(OC)=C2)=O)CCCC[C@H]1C(O[C@@H](C1=CC=CC(OCCN2CCOCC2)=C1)CCC1=CC=C(OC)C(OC)=C1)=O
SAfit2 Usage And Synthesis
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.
in vivo
It is found that 30 days of SAFit2 administration leads to a reduction in body weight under both control and high-fat diet (HFD) conditions. SAFit2 significantly increases phosphorylated AKT2 and AS160 in EDL muscle and likewise increases expression of GLUT4 at the membrane in soleus muscle[2]. When SAFit2 is applied 1 h before testing, no alterations in anxiety-related behavior are observed. However, SAFit2 treatment induces an anxiolytic phenotype in mice injected 16 h prior testing, which is reflected in a significantly increased open arm time in the elevated plus maze (EPM) (z=-2.183, p<0.05).? SAFit2 treatment leads to a significantly reduced latency to enter the lit compartment (z=-2 to 265, p<0.05), as well as a significantly increased distance traveled (t(20)=-2.371, p<0.05) in the lit compartment[3].
References
[1] STEFFEN GAALI. Selective inhibitors of the FK506-binding protein 51 by induced fit[J]. Nature chemical biology, 2014, 11 1: 33-37. DOI: 10.1038/nchembio.1699
[2] JAKOB HARTMANN. Pharmacological Inhibition of the Psychiatric Risk Factor FKBP51 Has Anxiolytic Properties.[J]. Journal of Neuroscience, 2015, 35 24: 9007-9016. DOI: 10.1523/jneurosci.4024-14.2015
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