1. Apoptosis
    Immunology/Inflammation
    Autophagy
  2. FKBP
  3. SAFit2

SAFit2 

Cat. No.: HY-102080 Purity: 98.59%
Handling Instructions

SAFit2 is a novel, selective FK506-binding protein 51 (FKBP51) antagonist with a Ki of 6 nM and also enhances AKT2-AS160 binding.

For research use only. We do not sell to patients.

SAFit2 Chemical Structure

SAFit2 Chemical Structure

CAS No. : 1643125-33-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 618 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg   Get quote  
50 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

SAFit2 is a novel, selective FK506-binding protein 51 (FKBP51) antagonist with a Ki of 6 nM and also enhances AKT2-AS160 binding.

IC50 & Target

Ki: 6 nM (FKBP51)[1]

In Vitro

SAFit2 is a novel, selective FK506-binding protein 51 (FKBP51) antagonist with a Ki of 6 nM in chemical assay and also enhances AKT2-AS160 binding[1]. 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[2].

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].

Molecular Weight

802.99

Formula

C₄₆H₆₂N₂O₁₀

CAS No.

1643125-33-0

SMILES

O=C(N1[[email protected]@H](CCCC1)C(O[[email protected]@H](C2=CC(OCCN3CCOCC3)=CC=C2)CCC4=CC(OC)=C(OC)C=C4)=O)[[email protected]@H](C5CCCCC5)C6=CC(OC)=C(OC)C(OC)=C6

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (155.67 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2453 mL 6.2267 mL 12.4535 mL
5 mM 0.2491 mL 1.2453 mL 2.4907 mL
10 mM 0.1245 mL 0.6227 mL 1.2453 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (2.59 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (2.59 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

Primary EDL myotubes are exposed to 0.6 µM SAFit2 or DMSO (vehicle) overnight. The following day, cells are serum-starved in low glucose (1000 mg/L) DMEM for 4 h with SAFit2 or DMSO, and are subsequently collected for the rapid preparation of the plasma membrane fraction. The membrane fraction is used in subsequent Western blot assays for the detection of GLUT4[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Male C57BL/6N mice at the age of 12 to 15 weeks are used. The mice are held under standard conditions (12 h light/dark cycle, lights on at 08:00 A.M.; temperature 23±2°C), are single housed and acclimatized to the room for 2 weeks before the commencing experiments. Food and tap water are available ad libitum. Animals receive a bilateral microinjection into the basolateral amygdala (BLA) (0.5 μL per side) of vehicle or SAFit2 (20 mg/kg BW) 16 h before the start of the test. The effects on anxiety-related behavior is analyzed (n=14 per group) 16 h after the application[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 98.59%

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