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SAFit2 Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5755498

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

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Product Documentation
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Sample Manual Insert View PDF
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Testing Data View PDF
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Certificate of Analysis (COA) View PDF
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QC Report View PDF
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Material Safety Data Sheet View PDF
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Technical Datasheet View PDF
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Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
SAFit2, Inhibitor
Full Product Name
SAFit2
Product Gene Name
SAFit2, inhibitor
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
802.99
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].

Structure of SAFit2, inhibitor

SAFit2 Inhibitor – Cat# MBS5755498

Product References and Citations for SAFit2, inhibitor

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.

Other Notes

Small volumes of SAFit2, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for SAFit2 purchase

MBS5755498 is an inhibitor targeting SAFit2.
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