SAFit2,1643125-33-0

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SAFit2

CAS No. : 1643125-33-0

MCE 国际站：SAFit2

产品活性：SAFit2 是一个高效且高选择性的 FK506 结合蛋白 51 (FKBP51) 抑制剂，其 K_i 值为 6 nM，并且能增强 AKT2-AS160 的结合。

研究领域：Apoptosis  |  Immunology/Inflammation  |  Autophagy

作用靶点：FKBP

In Vitro: SAFit2 treatment increases the expression of pAKT2 (soleus and EDL muscle) and pAS160 (EDL muscle) in WT cells, but there is no effect of FKBP51 antagonism in 51KO cells.? Moreover, following SAFit2 treatment, GLUT4 expression increases in the membrane fraction of primary EDL myotubes from WT mice, but not from 51KO 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. 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.

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