RO6806051
Based on 1 Customer Validation
RO6806051 is a selectivity FABP4 and FABP5 inhibitor with human FABP4 Ki values of 0.011 μM and 0.23 μM, and human FABP5 Ki values of 0.086 μM and 1.17 μM. RO6806051 can be used for the research of inflammation-related diseases.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.82%
- No. CAS: 1433901-75-7
- Fòrmula: C21H19ClN6
- Peso molecular:390.87
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 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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Immunology/Inflammation Compound Library
HY-L007
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Metabolism/Protease Compound Library
HY-L012
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Lipid Metabolism Compound Library
HY-L091
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Metabolic Enzyme Compound Library
HY-L146
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
Actividad biológica
RO6806051 acts as a potent dual inhibitor of purified human hFABP4 and hFABP5, with an ~209-fold selectivity for hFABP4 over hFABP3 and ~27-fold selectivity for hFABP5 over hFABP3[1].
RO6806051 (10 μM) has favorable physicochemical properties, low liver microsomal clearance in human and mouse, and weak to no inhibition of major cytochrome P450 enzymes at tested concentrations[1].
RO6806051 (10-80 μM; 24 h) exhibits significant cytotoxicity against differentiated THP-1 macrophages at concentrations of 20 μM and above[2].
RO6806051 (5-25 μM; 18 h pre-incubation before 6 h LPS stimulation) moderately inhibits MCP-1 secretion in LPS-stimulated THP-1 macrophages at concentrations of 5, 10, and 25 μM, with the highest inhibition at 25 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 human acute monocytic leukemia cells differentiated into macrophages
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Concentration:10-80 μM
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Incubation Time:24 h (after 24 h PMA differentiation)
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Result:Reduced cell viability of the control at 80 μM. Significantly inhibited cell viability at 20 μM.
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Cell Line:LPS-stimulated THP-1 macrophages
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Concentration:5-25 μM
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Incubation Time:18 h pre-incubation before 6 h LPS stimulation
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Result:Reduced LPS-induced MCP-1 secretion in a dose-dependent manner.
Chemical Information
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No. CAS 1433901-75-7
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Appearance Solid
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Peso molecular 390.87
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Fòrmula C21H19ClN6
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Color White to off-white
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SMILES
ClC1=CC2=C(N=C(N3CCCCC3)C(C4=NN=NN4)=C2C5=CC=CC=C5)C=C1
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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 : 125 mg/mL (319.80 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 (279 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]. Kühne H, et al. M. Design and synthesis of selective, dual fatty acid binding protein 4 and 5 inhibitors. Bioorg Med Chem Lett. 2016 Oct 15;26(20):5092-5097. [Content Brief]
[2]. He Y, et al. Discovery of Potent and Selective FABP4/5 Inhibitors with an Isoquinolone Scaffold as Potential Therapeutics for Inflammation-Related Diseases. J Med Chem. 2025;68(19):20207-20227. [Content Brief]
[3]. Chen S, et al. Recent Advances on Small-Molecule Inhibitors of Lipocalin-like Proteins. J Med Chem. 2024;67(7):5144-5167. [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 | 2.5584 mL | 12.7920 mL | 25.5840 mL | 63.9599 mL |
| 5 mM | 0.5117 mL | 2.5584 mL | 5.1168 mL | 12.7920 mL | |
| 10 mM | 0.2558 mL | 1.2792 mL | 2.5584 mL | 6.3960 mL | |
| 15 mM | 0.1706 mL | 0.8528 mL | 1.7056 mL | 4.2640 mL | |
| 20 mM | 0.1279 mL | 0.6396 mL | 1.2792 mL | 3.1980 mL | |
| 25 mM | 0.1023 mL | 0.5117 mL | 1.0234 mL | 2.5584 mL | |
| 30 mM | 0.0853 mL | 0.4264 mL | 0.8528 mL | 2.1320 mL | |
| 40 mM | 0.0640 mL | 0.3198 mL | 0.6396 mL | 1.5990 mL | |
| 50 mM | 0.0512 mL | 0.2558 mL | 0.5117 mL | 1.2792 mL | |
| 60 mM | 0.0426 mL | 0.2132 mL | 0.4264 mL | 1.0660 mL | |
| 80 mM | 0.0320 mL | 0.1599 mL | 0.3198 mL | 0.7995 mL | |
| 100 mM | 0.0256 mL | 0.1279 mL | 0.2558 mL | 0.6396 mL |
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