Netoglitazone
Based on 1 Customer Validation
Netoglitazone (MCC-555) is an orally active PPARγ ligand with an EC50 of 8 μM. Netoglitazone mediates cell type-specific functional regulation, and modulates the transcriptional activity of PPARγ as a full agonist, partial agonist or antagonist. Netoglitazone induces adipogenesis, inhibits osteoblastogenesis, alters the weight of extramedullary fat depots and enhances insulin sensitivity. Netoglitazone reduces blood glucose levels. Netoglitazone can be used in research related to type 2 diabetes and non-insulin-dependent diabetes mellitus.
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- Pureza: 99.92%
- No. CAS: 161600-01-7
- Fòrmula: C21H16FNO3S
- Peso molecular:381.42
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
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Actividad biológica
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PPARγ |
Netoglitazone (0.01-10 μM) induces the differentiation of U-33/γ2 cells into adipocytes in a concentration-dependent manner in vitro[1].
Netoglitazone (0.01-10 μM; 6 days) inhibits alkaline phosphatase activity in U-33/γ2 cells. A concentration higher than 1 μM is required for complete inhibition, and its potency after 6 days of treatment is at least 250-fold lower than that of rosiglitazone[1].
Netoglitazone (0.01-10 μM; 6 days) inhibits osteoblast mineralization in U-33/γ2 cells[1].
Netoglitazone (2 h) binds to PPARγ with an EC50 of 8 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:murine marrow-derived U-33/γ2 cells
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Concentration:2.5 μM
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Incubation Time:3 days
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Result:Elevated FABP4/aP2 mRNA levels (adipocyte marker) at 2.5 μM.
Almost completely suppressed Runx2 mRNA levels (osteoblast marker) at 2.5 μM.
Matched the phenotypic effects of 0.5 μM rosiglitazone.
Netoglitazone maleate (10 μg/g body weight/day; oral administration; daily dosing for 7 weeks) alters fat depot weight and promotes bone marrow adipogenesis in non-diabetic male C57BL/6 mice, without affecting their trabecular bone microstructure or osteoblast gene expression, while causing a slight reduction in whole-body bone mineral content (BMC)[1].
Netoglitazone (1-30 mg/kg/day; p.o.; daily; for 4 consecutive days) potently reduces plasma glucose levels in obese diabetic KK-Ay mice, with an ED25 of 2.7 mg/kg/day, and regulates the expression of PPARγ-responsive genes in adipose tissue[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (6-month-old male, non-diabetic)[1]
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Dosage:10 μg/g body weight/day
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Administration:p.o.; daily; 7 weeks
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Result:Did not affect body weight or blood glucose levels.
Decreased epididymal white adipose tissue (WAT) weight by 32.2%.
Increased interscapular brown adipose tissue (BAT) weight by 47.8%.
Left whole body bone mineral density (BMD) unchanged, but decreased whole body bone mineral content (BMC) by 4.6%.
Showed no changes in trabecular bone microarchitecture parameters (BV/TV, Tb.Th., Tb.N., Tb.Sp., Conn.D., SMI, DA) in the proximal tibia.
Increased marrow adipocyte number in the proximal tibia 3- to 6-fold.
Left expression of osteoblast-specific genes (Runx2, Dlx5, osteocalcin, α1(I) collagen) in the tibia unaffected, while increased adipocyte-specific gene FABP4/aP2 expression was increased 1.8-fold.
Chemical Information
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No. CAS 161600-01-7
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Appearance Solid
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Peso molecular 381.42
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Fòrmula C21H16FNO3S
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Color White to yellow
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SMILES
O=C(N1)SC(CC2=CC=C3C=C(OCC4=CC=CC=C4F)C=CC3=C2)C1=O
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Synonyms
MCC-555; Isaglitazone
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 250 mg/mL (655.45 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)
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 (5.45 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 (5.45 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.
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 (277 KB)
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SDS (458 KB)
- English - EN (458 KB)
- Français - FR (458 KB)
- Deutsch - DE (458 KB)
- Norwegian - NO (458 KB)
- Español - ES (458 KB)
- Swedish - SV (458 KB)
- Italian - IT (458 KB)
- Korean - KR (458 KB)
- Portuguese - PT (458 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Lazarenko OP, et al. Netoglitazone is a PPAR-gamma ligand with selective effects on bone and fat. Bone. 2006;38(1):74-84. [Content Brief]
[2]. Grey A, et al. Skeletal consequences of thiazolidinedione therapy. Osteoporos Int. 2008;19(2):129-137. [Content Brief]
[3]. Reginato MJ, et al. A potent antidiabetic thiazolidinedione with unique peroxisome proliferator-activated receptor gamma-activating properties. J Biol Chem. 1998;273(49):32679-32684. [Content Brief]
[4]. Ramakers JD, et al. The PPARgamma agonist rosiglitazone impairs colonic inflammation in mice with experimental colitis. J Clin Immunol. 2007;27(3):275-283. [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 | 2.6218 mL | 13.1089 mL | 26.2178 mL | 65.5445 mL |
| 5 mM | 0.5244 mL | 2.6218 mL | 5.2436 mL | 13.1089 mL | |
| 10 mM | 0.2622 mL | 1.3109 mL | 2.6218 mL | 6.5545 mL | |
| 15 mM | 0.1748 mL | 0.8739 mL | 1.7479 mL | 4.3696 mL | |
| 20 mM | 0.1311 mL | 0.6554 mL | 1.3109 mL | 3.2772 mL | |
| 25 mM | 0.1049 mL | 0.5244 mL | 1.0487 mL | 2.6218 mL | |
| 30 mM | 0.0874 mL | 0.4370 mL | 0.8739 mL | 2.1848 mL | |
| 40 mM | 0.0655 mL | 0.3277 mL | 0.6554 mL | 1.6386 mL | |
| 50 mM | 0.0524 mL | 0.2622 mL | 0.5244 mL | 1.3109 mL | |
| 60 mM | 0.0437 mL | 0.2185 mL | 0.4370 mL | 1.0924 mL | |
| 80 mM | 0.0328 mL | 0.1639 mL | 0.3277 mL | 0.8193 mL | |
| 100 mM | 0.0262 mL | 0.1311 mL | 0.2622 mL | 0.6554 mL |
Netoglitazone Related Classifications
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