Art. -Nr.: HY-102080

SAFit2

9 Cited Publications

Kundenbewertung

Based on 9 publication(s) in Google Scholar

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

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Reinheit: 99.24%
CAS. Nr.: 1643125-33-0
Formel: C₄₆H₆₂N₂O₁₀
Molecular Weight:802.99

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

SAFit2 Chemical Structure

CAS. Nr.: 1643125-33-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (9)
Lösungsmittel & Löslichkeit
- In Vitro
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

SAFit2, a chemical probe, is a highly potent, highly selective FK506-binding protein 51 (FKBP51) inhibitor with a K_i 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.

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.

Chemical Information

CAS. Nr. 1643125-33-0
Appearance Solid
Molecular Weight 802.99
Formel C₄₆H₆₂N₂O₁₀
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (9)

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Journal Impact Factor

Nat Metab

Pathogenic role of acyl coenzyme A binding protein (ACBP) in Cushing's syndrome. [Abstract]

2024 Dec;6(12):2281-2299. PMID: 39578649

SAFit2 purchased from MedChemExpress. Usage Cited in: Nat Metab. 2024 Dec;6(12):2281-2299. [Abstract]

Mice were fasted or received HCS (100 mg /kg; i.p.) for 24 h combined with SAFit2 (40 mg /kg; i.p.) or vehicle, and plasma ACBP was measured by ELISA.
Cell Discov

Psychological stress-induced systemic corticosterone directly sabotages intestinal stem cells and exacerbates colitis. [Abstract]

2025 May 13;11(1):46. PMID: 40360481

SAFit2 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2025 May 13;11(1):46. [Abstract]

Representative images of day 4 organoids after ex vivo treatment with 200 μM CORT, 0.25 μM SAFit2, or 200 μM CORT supplemented with 0.25 μM SAFit2.

SAFit2 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2025 May 13;11(1):46. [Abstract]

Western blotting for AKT and pAKT (S473) in the small intestinal crypts of the vehicle-treated, SAFit2-treated (20 mg/kg/day) mice.
Int J Biol Macromol

FKBP5 inhibitor suppresses platelet activation and thrombosis by inhibiting IKBKE/PI3K/Rap1 pathway. [Abstract]

2025 May 7:144068. PMID: 40345291
Free Radic Biol Med

Hyperactivation of the m6A demethylase FTO to down-regulate SLC7A11/xCT-mediated redox homeostasis and epigenetic remodeling in facial infiltrating lipomatosis. [Abstract]

2025 Nov:239:432-448. PMID: 40769313
Free Radic Biol Med

FKBP5 regulates trophoblast-macrophage crosstalk in recurrent spontaneous abortion through PI3K/AKT and NF-κB signaling pathways. [Abstract]

2023 Oct 10;209(Pt 1):55-69. PMID: 37827456
J Steroid Biochem Mol Biol

Corticosterone mediates FKBP51 signaling and inflammation response in the trigeminal ganglion in chronic stress-induced corneal hyperalgesia mice. [Abstract]

2023 Jul:231:106312. PMID: 37062346
Biochim Biophys Acta Proteins Proteom

Propagation of conformational instability in FK506-binding protein FKBP12. [Abstract]

2024 May 1;1872(3):140990. PMID: 38142946
Scand J Immunol

Novel immunosuppressive effect of FK506 by upregulation of PD-L1 via FKBP51 in heart transplantation. [Abstract]

2022 Jul 8;e13203. PMID: 35801698
SSRN

2025 Apr 12.

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Protokoll

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].

MedChemExpress (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].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. 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. [Content Brief]

[2]. Balsevich G, et al. Stress-responsive FKBP51 regulates AKT2-AS160 signaling and metabolic function. Nat Commun. 2017 Nov 23;8(1):1725. [Content Brief]

[3]. Hartmann J, et al. Pharmacological Inhibition of the Psychiatric Risk Factor FKBP51 Has Anxiolytic Properties. J Neurosci. 2015 Jun 17;35(24):9007-16. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

SAFit2

9 Cited Publications

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SAFit2

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) SAFit2

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SAFit2

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) SAFit2

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SAFit2 Related Classifications

HY-102080 Related Classifications