TUG-469
Based on 1 Customer Validation
TUG-469 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.67%
- No. CAS: 1236109-67-3
- Fòrmula: C23H23NO2
- Peso molecular:345.43
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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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
In Vitro
TUG-469 (0-10 μM) shows efficacy to hFFA1 with a pEC50 value of 7.73[1]. TUG-469 (10 μM) increases the insulin secretion under 10 mM glucose stimulation[1]. TUG-469 (0-100 μM) is >200-fold selective for FFA1 over FFA4 with EC50 values of 19 nM and 4.4 μM for FFA1 and FFA4, respectively[2]. TUG-469 (5 μM; 30 min) significantly increases insulin secretion of INS-1 cells with the presence of high glucose concentration (16.7 mM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male NZO mice with glucose administration[2]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection; 5 mg/kg; 60 and 90 min after glucose administration
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Result:Reduced the blood glucose level.
Chemical Information
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No. CAS 1236109-67-3
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Appearance Solid
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Peso molecular 345.43
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Fòrmula C23H23NO2
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Color White to off-white
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SMILES
O=C(CCC1=CC=C(C=C1)NCC2=CC(C3=CC=CC=C3C)=CC=C2)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
In Vitro:
DMSO : 100 mg/mL (289.49 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)
Protocolo
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Pureza y Documentación
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Ficha de datos (270 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Christiansen E, et al. Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. ACS Med Chem Lett. 2010 Jul 2;1(7):345-9. [Content Brief]
[2]. Urban C, et al. In vitro and mouse in vivo characterization of the potent free fatty acid 1 receptor agonist TUG-469. Naunyn Schmiedebergs Arch Pharmacol. 2013 Dec;386(12):1021-30. [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 | 2.8949 mL | 14.4747 mL | 28.9494 mL | 72.3736 mL |
| 5 mM | 0.5790 mL | 2.8949 mL | 5.7899 mL | 14.4747 mL | |
| 10 mM | 0.2895 mL | 1.4475 mL | 2.8949 mL | 7.2374 mL | |
| 15 mM | 0.1930 mL | 0.9650 mL | 1.9300 mL | 4.8249 mL | |
| 20 mM | 0.1447 mL | 0.7237 mL | 1.4475 mL | 3.6187 mL | |
| 25 mM | 0.1158 mL | 0.5790 mL | 1.1580 mL | 2.8949 mL | |
| 30 mM | 0.0965 mL | 0.4825 mL | 0.9650 mL | 2.4125 mL | |
| 40 mM | 0.0724 mL | 0.3619 mL | 0.7237 mL | 1.8093 mL | |
| 50 mM | 0.0579 mL | 0.2895 mL | 0.5790 mL | 1.4475 mL | |
| 60 mM | 0.0482 mL | 0.2412 mL | 0.4825 mL | 1.2062 mL | |
| 80 mM | 0.0362 mL | 0.1809 mL | 0.3619 mL | 0.9047 mL | |
| 100 mM | 0.0289 mL | 0.1447 mL | 0.2895 mL | 0.7237 mL |
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