AS1708727
Based on 3 publication(s) in Google Scholar
AS1708727 is an orally active Foxo1 inhibitor, with EC50 values of 0.33 μM and 0.59 μM for G6Pase and PEPCK, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.44%
- No. CAS: 1253226-93-5
- Fòrmula: C24H24Cl2N2O2
- Peso molecular:443.37
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) AS1708727
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Actividad biológica
Descripciòn
In Vitro
AS1708727 suppresses increases in blood glucose level by inhibiting gluconeogenic gene expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Fao cells, derived from the H4IIE hepatoma cell line.
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Concentration:0.1-3000 μM.
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Incubation Time:18 h.
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Result:Showed dose-dependent reduction in mRNA levels for G6Pase and PEPCK.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:db/db mice aged six weeks[1].
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Dosage:100-1000 mg/kg (Pharmacokinetic Analysis).
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Administration:Orally.
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Result:Cmax) was 26.7 μM and maximum drug concentration time (Tmax) of 0.5 h at 300 mg/kg[1].
Liver concentration of AS1708727 at 0.5-2 h after oral administration was 3.7- to 5.4-fold higher than the plasma concentration, indicating good liver transition of AS1708727[1].
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Animal Model:Diabetic model mice[1].
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Dosage:30 to 300 mg/kg.
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Administration:Orally twice daily for 4 days.
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Result:Blood glucose level was significantly reduced at 300 mg/kg[1].
Plasma alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels were significantly reduced at 300 mg/kg[1].
G6Pase and PEPCK mRNA levels were significantly reduced at dosages of 100 and 300 mg/kg[1].
Chemical Information
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No. CAS 1253226-93-5
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Appearance Solid
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Peso molecular 443.37
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Fòrmula C24H24Cl2N2O2
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Color White to off-white
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SMILES
O=C(CC1CCCC1)N(C)C2=CC=C(C(COC3=CC=CC4=C3C=CN=C4)=C2Cl)Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Phytomedicine
Baizhu shaoyao decoction restores the intestinal barrier and brain-gut axis balance to alleviate diarrhea-predominant irritable bowel syndrome via FoxO1/FoxO3a. [Abstract]2024 Jan:122:155163. PMID: 37924689 -
iScience
2023 Jul 11;26(8):107293. PMID: 37520709 -
FEBS Open Bio
The FOXO1 inhibitor AS1842856 triggers apoptosis in glioblastoma multiforme and basal-like breast cancer cells. [Abstract]2023 Feb;13(2):352-362. PMID: 36602390
Solvente y solubilidad
In Vitro:
DMSO : 41.67 mg/mL (93.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.69 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.69 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.2555 mL | 11.2773 mL | 22.5545 mL | 56.3863 mL |
| 5 mM | 0.4511 mL | 2.2555 mL | 4.5109 mL | 11.2773 mL | |
| 10 mM | 0.2255 mL | 1.1277 mL | 2.2555 mL | 5.6386 mL | |
| 15 mM | 0.1504 mL | 0.7518 mL | 1.5036 mL | 3.7591 mL | |
| 20 mM | 0.1128 mL | 0.5639 mL | 1.1277 mL | 2.8193 mL | |
| 25 mM | 0.0902 mL | 0.4511 mL | 0.9022 mL | 2.2555 mL | |
| 30 mM | 0.0752 mL | 0.3759 mL | 0.7518 mL | 1.8795 mL | |
| 40 mM | 0.0564 mL | 0.2819 mL | 0.5639 mL | 1.4097 mL | |
| 50 mM | 0.0451 mL | 0.2255 mL | 0.4511 mL | 1.1277 mL | |
| 60 mM | 0.0376 mL | 0.1880 mL | 0.3759 mL | 0.9398 mL | |
| 80 mM | 0.0282 mL | 0.1410 mL | 0.2819 mL | 0.7048 mL |
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