OPC-163493
Based on 1 Customer Validation
OPC-163493 is an orally active and liver-targeted mitochondrial uncoupling agent. OPC-163493 reduces the production of mitochondrial Δψ and ROS. OPC-163493 has anti-diabetic and lipid-lowering effects. In addition, OPC-163493 has a protective effect on cardiovascular disease.
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- Pureza: 99.34%
- No. CAS: 1644467-84-4
- Fòrmula: C14H8F3N5S
- Peso molecular:335.31
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Almacenamiento:Powder -20°C, 3 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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Actividad biológica
OPC-163493 (0.5-10 μM; 15 min) inhibits the production of Δψ and ROS in isolated rat liver mitochondria[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
OPC-163493 (1-10 mg/kg; Oral administration; 6 weeks) has an improved effect in diabetic rat model[1].
OPC-163493 (2-4 mg/kg; Oral administration; 2 weeks) has a lipid-lowering effect in rat models with high fat diet[1].
OPC-163493 (0.06% mixed chow; 51 days) has a protective effect in spontaneously hypertensive rat models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Zucker diabetic fatty rats aged 11 weeks old[1]
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Dosage:1, 2, 4 and 10 mg/kg
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Administration:Oral administration (p.o.); 6 weeks
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Result:Suppressed HbA1c elevation in a dose-dependent manner.
Significantly lowered fasting blood glucose levels at doses of 4 and 10 mg/kg.
Had no significant effect on plasma insulin levels.
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Animal Model:HFD SD rats aged 12 weeks old[1]
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Dosage:2 and 4 mg/kg
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Administration:Oral administration (p.o.); 2 weeks
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Result:Did not affect body weight and food intake during the treatment period.
Slightly but significantly reduced fasting blood glucose after 2-week treatment.
Significantly reduced hepatic total TG, total diacylglycerol (DAG), and total cholesterol ester (CE) by 57%, 25%, and 26%, respectively even in the low-dose group.
Significantly reduced long-chain acylcarnitines (AC, C16 and C18).
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Animal Model:Salt-loaded stroke-prone spontaneously hypertensive rats (SHRSPs) aged 6 weeks old[1]
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Dosage:0.06% mixed chow
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Administration:Oral administration (p.o.); 51 days
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Result:Delayed stroke symptoms and death, lowered blood pressure.
Improved kidney function and urinary albumin-to-creatinine ratio, lowered uinary albumin excretion by 68%.
Chemical Information
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No. CAS 1644467-84-4
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Appearance Solid
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Peso molecular 335.31
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Fòrmula C14H8F3N5S
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Color White to off-white
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SMILES
N#CC1=C(C2=C(C)SC(C3=CC=C(C(F)(F)F)C=C3)=N2)N=NN1
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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 : 125 mg/mL (372.79 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)
Pureza y Documentación
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Ficha de datos (274 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]. Kanemoto N, et al. Antidiabetic and cardiovascular beneficial effects of a liver-localized mitochondrial uncoupler. Nat Commun. 2019 May 15;10(1):2172. [Content Brief]
[2]. Inoue Y, et al. Preclinical safety profile of a liver-localized mitochondrial uncoupler: OPC-163493. EXCLI J. 2022 Jan 11;21:213-235. [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 | 2.9823 mL | 14.9116 mL | 29.8231 mL | 74.5579 mL |
| 5 mM | 0.5965 mL | 2.9823 mL | 5.9646 mL | 14.9116 mL | |
| 10 mM | 0.2982 mL | 1.4912 mL | 2.9823 mL | 7.4558 mL | |
| 15 mM | 0.1988 mL | 0.9941 mL | 1.9882 mL | 4.9705 mL | |
| 20 mM | 0.1491 mL | 0.7456 mL | 1.4912 mL | 3.7279 mL | |
| 25 mM | 0.1193 mL | 0.5965 mL | 1.1929 mL | 2.9823 mL | |
| 30 mM | 0.0994 mL | 0.4971 mL | 0.9941 mL | 2.4853 mL | |
| 40 mM | 0.0746 mL | 0.3728 mL | 0.7456 mL | 1.8639 mL | |
| 50 mM | 0.0596 mL | 0.2982 mL | 0.5965 mL | 1.4912 mL | |
| 60 mM | 0.0497 mL | 0.2485 mL | 0.4971 mL | 1.2426 mL | |
| 80 mM | 0.0373 mL | 0.1864 mL | 0.3728 mL | 0.9320 mL | |
| 100 mM | 0.0298 mL | 0.1491 mL | 0.2982 mL | 0.7456 mL |
OPC-163493 Related Classifications
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