SBI-477
Based on 1 publication(s) in Google Scholar
SBI-477 is a chemical probe that stimulates insulin signaling by deactivating the transcription factor MondoA. SBI-477 can lead to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain-containing 4 (ARRDC4). SBI-477 coordinately inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes.
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- Pureza: 98.0%
- No. CAS: 781628-99-7
- Fòrmula: C24H25N3O6S
- Peso molecular:483.54
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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) SBI-477
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Actividad biológica
MondoA[1]
SBI-477 shows potent inhibition of TAG accumulation in rat H9c2 myocytes (EC50 = 100 nM) and human skeletal myotubes (EC50 = 1 μM)[1].
SBI-477 (10 μM, 24 h) leads to a marked reduction of 18:1 species and levels of TAG and DAG species[1].
SBI-477 markedly reduces the contribution by the de novo glycerolphosphate biosynthetic pathway (K1), and results in a shift to the monoacylglycerol reacylation pathway (K2)[1].
SBI-477 (0.3-10 μM, 24 h) increases both basal and insulin-stimulated glucose uptake, and enhances glycogen synthesis rates in human skeletal myotubes[1].
SBI-477 (10 μM, 16 h) inhibits glucose-stimulated Arrdc4 and Txnip and increases glucose uptake in a dose-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human skeletal myotubes
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Concentration:10 μM
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Incubation Time:24 h
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Result:Resulted in near-complete nuclear exclusion of MondoA.
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Cell Line:Human skeletal myotubes
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Concentration:0.3, 1, 3, and 10 μM
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Incubation Time:24 h
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Result:Increased the tyrosine phosphorylation of the insulin receptor substrate-1 (IRS-1).
Decreased IRS-1 phosphorylation at serine sites 636 and 639.
Increased the phosphorylation of the downstream effector kinase Akt.
Reduced TXNIP protein levels in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week-old male C57BL/6J mice with diet-induced obesity[1]
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Dosage:50 mg/kg
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Administration:Subcutaneous injection (s.c.) once daily for 7 days
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Result:Resulted in a small but significant reduction in body weight compared to vehicle.
Reduced expression of TAG synthesis and lipogenic genes in both muscle and liver.
Chemical Information
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No. CAS 781628-99-7
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Appearance Solid
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Peso molecular 483.54
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Fòrmula C24H25N3O6S
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Color Light yellow to yellow
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SMILES
O=C(NC1=NC(C2=CC=C(OC)C=C2)=CS1)C3=CC=C(OCC(N4CCOCC4)=O)C(OC)=C3
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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 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
MAX inactivation deregulates the MYC network and induces neuroendocrine neoplasia in multiple tissues. [Abstract]2024 Sep 24:2024.09.21.614255. PMID: 39386474
Solvente y solubilidad
DMSO : 65 mg/mL (134.43 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.17 mg/mL (4.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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: ≥ 2.17 mg/mL (4.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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.
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 (276 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
[1]. Ahn B, et al. MondoA coordinately regulates skeletal myocyte lipid homeostasis and insulin signaling. J Clin Invest. 2016 Sep 1;126(9):3567-79. [Content Brief]
[2]. Nakayama, Y., et al., (2024). Systemic Deletion of ARRDC4 Improves Cardiac Reserve and Exercise Capacity in Diabetes. Circulation research, 135(3), 416–433. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0681 mL | 10.3404 mL | 20.6808 mL | 51.7020 mL |
| 5 mM | 0.4136 mL | 2.0681 mL | 4.1362 mL | 10.3404 mL | |
| 10 mM | 0.2068 mL | 1.0340 mL | 2.0681 mL | 5.1702 mL | |
| 15 mM | 0.1379 mL | 0.6894 mL | 1.3787 mL | 3.4468 mL | |
| 20 mM | 0.1034 mL | 0.5170 mL | 1.0340 mL | 2.5851 mL | |
| 25 mM | 0.0827 mL | 0.4136 mL | 0.8272 mL | 2.0681 mL | |
| 30 mM | 0.0689 mL | 0.3447 mL | 0.6894 mL | 1.7234 mL | |
| 40 mM | 0.0517 mL | 0.2585 mL | 0.5170 mL | 1.2926 mL | |
| 50 mM | 0.0414 mL | 0.2068 mL | 0.4136 mL | 1.0340 mL | |
| 60 mM | 0.0345 mL | 0.1723 mL | 0.3447 mL | 0.8617 mL | |
| 80 mM | 0.0259 mL | 0.1293 mL | 0.2585 mL | 0.6463 mL | |
| 100 mM | 0.0207 mL | 0.1034 mL | 0.2068 mL | 0.5170 mL |
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