SAFit2
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 Ki of 6 nM and also enhances AKT2-AS160 binding.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.24%
- CAS 番号: 1643125-33-0
- 分子式: C46H62N2O10
- 分子量:802.99
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 SAFit2
More- Nat Metab. 2024 Dec;6(12):2281-2299. [Abstract]
- Cell Discov. 2025 May 13;11(1):46. [Abstract]
- Int J Biol Macromol. 2025 May 7:144068. [Abstract]
- Free Radic Biol Med. 2025 Nov:239:432-448. [Abstract]
- Free Radic Biol Med. 2023 Oct 10;209(Pt 1):55-69. [Abstract]
- J Steroid Biochem Mol Biol. 2023 Jul:231:106312. [Abstract]
- Biochim Biophys Acta Proteins Proteom. 2024 May 1;1872(3):140990. [Abstract]
- Scand J Immunol. 2022 Jul 8;e13203. [Abstract]
- SSRN. 2025 Apr 12.
Customer Validation & Images
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ELISA
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Cell Imaging/Staining
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WB
生物活性
Ki: 6 nM (FKBP51)[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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1643125-33-0
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性状 Solid
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分子量 802.99
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分子式 C46H62N2O10
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Color Off-white to pink
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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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (9)
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Journal Impact Factor
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Most Recent
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Nat Metab
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.
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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.
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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
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 -
溶剤 & 溶解度
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.
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
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.
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.
純度とドキュメンテーション
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データシート (282 KB)
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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)
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取扱説明書 (2659 KB)
参考文献
[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]
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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