2. Apoptosis Immunology/Inflammation Cell Cycle/DNA Damage Autophagy
  3. FKBP
  4. SAFit2

SAFit2 est un inhibiteur de la protéine de liaison FK506 51 (FKBP51) qui est très puissant et très sélectif avec un Ki de 6 nM et améliore également la liaison AKT2-AS160.

SAFit2, a chemical probe, is a highly potent, highly selective FK506-binding protein 51 (FKBP51) inhibitor with a Ki of 6 nM and also enhances AKT2-AS160 binding.

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

SAFit2

SAFit2 Chemical Structure

CAS No. : 1643125-33-0

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Based on 9 publication(s) in Google Scholar

SAFit2 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

SAFit2, a chemical probe, is a highly potent, highly selective FK506-binding protein 51 (FKBP51) inhibitor with a Ki of 6 nM and also enhances AKT2-AS160 binding[1].

IC50 & Target

Ki: 6 nM (FKBP51)[1]
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[2].

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

SAFit2 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

802.99

Formula

C46H62N2O10
CAS No.
Appearance

Solid

Color

Off-white to pink

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
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 : ≥ 100 mg/mL (124.53 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2453 mL 6.2267 mL 12.4535 mL 31.1336 mL
5 mM 0.2491 mL 1.2453 mL 2.4907 mL 6.2267 mL
10 mM 0.1245 mL 0.6227 mL 1.2453 mL 3.1134 mL
15 mM 0.0830 mL 0.4151 mL 0.8302 mL 2.0756 mL
20 mM 0.0623 mL 0.3113 mL 0.6227 mL 1.5567 mL
25 mM 0.0498 mL 0.2491 mL 0.4981 mL 1.2453 mL
30 mM 0.0415 mL 0.2076 mL 0.4151 mL 1.0378 mL
40 mM 0.0311 mL 0.1557 mL 0.3113 mL 0.7783 mL
50 mM 0.0249 mL 0.1245 mL 0.2491 mL 0.6227 mL
60 mM 0.0208 mL 0.1038 mL 0.2076 mL 0.5189 mL
80 mM 0.0156 mL 0.0778 mL 0.1557 mL 0.3892 mL
100 mM 0.0125 mL 0.0623 mL 0.1245 mL 0.3113 mL
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SAFit2 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SAFit21643125-33-0SAFit 2SAFit-2FKBPFK506-binding proteinInhibitorinhibitorinhibit

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SAFETY DATA SHEET (SDS)

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