SAFit2, inhibitor

SAFit2

Cat. Num. AAA5755498

• Purity: 98.00%
• Synonyms: SAFit2; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 125mg/mL (155.67mM) Need ultrasonic; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C46H62N2O10
• SMILES: O=C(N1[C@@H](CCCC1)C(O[C@@H](C2=CC(OCCN3CCOCC3)=CC=C2)CCC4=CC(OC)=C(OC)C=C4)=O)[C@@H](C5CCCCC5)C6=CC(OC)=C(OC)C(OC)=C6
• CAS Number: 1643125-33-0
• Target & IC50: FKBP51: ic50 6nM (ki)
• In Vitro: SAFit2 significantly increases phosphorylated AKT2 and AS160 in EDL muscle and likewise increases expression of GLUT4 at the membrane in soleus muscle. 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. It is found that 30 days of SAFit2 administration leads to a reduction in body weight under both control and high-fat diet conditions. When SAFit2 is applied 1 h before testing, no alterations in anxiety-related behavior are observed [2][3].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for SAFit2, inhibitor

SAFit2 is a highly potent and selective FK506-binding protein 51 inhibitor (Ki: 6nM) and also enhances AKT2-AS160 binding.

References

Gaali S, et al. Rapid, Structure-Based Exploration of Pipecolic Acid Amides as Novel Selective Antagonists of the FK506-Binding Protein 5J Med Chem. 2016 Mar 24;59(6):2410-22.
Gaali S, et al. Rapid, Structure-Based Exploration of Pipecolic Acid Amides as Novel Selective Antagonists of the FK506-Binding Protein 51. J Med Chem. 2016 Mar 24;59(6):2410-22.
Balsevich G, et al. Stress-responsive FKBP51 regulates AKT2-AS160 signaling and metabolic function. Nat Commun. 2017 Nov 23;8(1):1725.
Balsevich G, et al. Stress-responsive FKBP51 regulates AKT2-AS160 signaling and metabolic function. Nat Commun. 2017 Nov 23;8(1):1725.
Hartmann J, et al. Pharmacological Inhibition of the Psychiatric Risk Factor FKBP51 Has Anxiolytic Properties. J Neurosci. 2015 Jun 17;35(24):9007-16.
Hartmann J, et al. Pharmacological Inhibition of the Psychiatric Risk Factor FKBP51 Has Anxiolytic Properties. J Neurosci. 2015 Jun 17;35(24):9007-16.