FK614
Based on 1 Customer Validation
FK614 is an orally active, non-thiazolidinedione (TZD) type, and selective PPARγ modulator (SPPARM). FK614 functions as a PPARγ agonist with potent anti-diabetic activity in vivo. FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 can be used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.97%
- No. CAS: 193012-35-0
- Fòrmula: C21H23Cl2N3O3S
- Peso molecular:468.40
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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
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Actividad biológica
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PPAR-γ |
FK614 (0.1~10000 nM; 24 hours; CV-1 cells) activates PPARγ-dependent transcription in a concentration-dependent manner. FK614 (0~0.1 μM; 5 days; 3T3-L1 adipocytes) makes triglyceride content increased in a concentration-dependent manner. FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation[1].
FK614 is an insulin sensitizer potentially for treatment of postherpetic neuralgia. FK614 is a non-TZD insulin sensitizer[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
FK614 (0.1~10 mg/kg; p.o.; 14 days) improves the impaired glucose tolerance[3].
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
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Dosage:0.1~10 mg/kg
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Administration:P.o.
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Result:Improved the impaired glucose tolerance.
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Animal Model:db/db Mice
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Dosage:0.32~3.2 mg/kg
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Administration:P.o.
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Result:Dose-dependently reduced plasma glucose level.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 193012-35-0
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Appearance Solid
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Peso molecular 468.40
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Fòrmula C21H23Cl2N3O3S
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Color White to off-white
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SMILES
O=C(C1=CC=C2N=C(C)N(CC3=CC=C(Cl)C=C3Cl)C2=C1)NS(=O)(CCCCC)=O
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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
Solvente y solubilidad
DMSO : 100 mg/mL (213.49 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.
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 (272 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]. Fujimura T, et al. A selective peroxisome proliferator-activated receptor gamma modulator with distinct fat cell regulation properties. J Pharmacol Exp Ther. 2006;318(2):863-871. [Content Brief]
[2]. Fujimura T, et al. FK614, a novel peroxisome proliferator-activated receptor gamma modulator, induces differential transactivation through a unique ligand-specific interaction with transcriptional coactivators. J Pharmacol Sci. 2005;99(4):342-352. [Content Brief]
[3]. Minoura H, et al. Ameliorating effect of FK614, a novel nonthiazolidinedione peroxisome proliferator-activated receptor gamma agonist, on insulin resistance in Zucker fatty rat. Eur J Pharmacol. 2005;519(1-2):182-190. [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 | 2.1349 mL | 10.6746 mL | 21.3493 mL | 53.3732 mL |
| 5 mM | 0.4270 mL | 2.1349 mL | 4.2699 mL | 10.6746 mL | |
| 10 mM | 0.2135 mL | 1.0675 mL | 2.1349 mL | 5.3373 mL | |
| 15 mM | 0.1423 mL | 0.7116 mL | 1.4233 mL | 3.5582 mL | |
| 20 mM | 0.1067 mL | 0.5337 mL | 1.0675 mL | 2.6687 mL | |
| 25 mM | 0.0854 mL | 0.4270 mL | 0.8540 mL | 2.1349 mL | |
| 30 mM | 0.0712 mL | 0.3558 mL | 0.7116 mL | 1.7791 mL | |
| 40 mM | 0.0534 mL | 0.2669 mL | 0.5337 mL | 1.3343 mL | |
| 50 mM | 0.0427 mL | 0.2135 mL | 0.4270 mL | 1.0675 mL | |
| 60 mM | 0.0356 mL | 0.1779 mL | 0.3558 mL | 0.8896 mL | |
| 80 mM | 0.0267 mL | 0.1334 mL | 0.2669 mL | 0.6672 mL | |
| 100 mM | 0.0213 mL | 0.1067 mL | 0.2135 mL | 0.5337 mL |
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