DG051
Based on 1 publication(s) in Google Scholar
DG051 is a potent leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis in the enzyme assay with an IC50=47 nM.
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- Pureza: 99.86%
- No. CAS: 929915-58-2
- Fòrmula: C21H25Cl2NO4
- Peso molecular:426.33
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Publications Citing Use of MedChemExpress (MCE) DG051
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Actividad biológica
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LTA4H hydrolase |
DG051 is a potent inhibitor of LTA4H aminopeptidase activity against L-alanine p-nitroanilide (IC50=72 nM). DG051 inhibits human whole blood (HWB) with IC50 of 37 nM. As applied within the context of LTA4H inhibitor design, the chemistry team is able to design a potent DG051(Kd=26 nM) with high aqueous solubility (>30 mg/mL) and high oral bioavailability (>80% across species) that is currently undergoing clinical evaluation for the treatment of myocardial infarction and stroke[1] DG-051 is a first-in-class small molecule inhibitor of leukotriene A4 hydrolase (LTA4H), currently in Phase II clinical development for the prevention of heart attack[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 929915-58-2
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Appearance Solid
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Peso molecular 426.33
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Fòrmula C21H25Cl2NO4
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Color White to light yellow
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SMILES
Cl[H].O=C(O)CCCN1CCC[C@H]1COC(C=C2)=CC=C2OC3=CC=C(Cl)C=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
DMSO : ≥ 325 mg/mL (762.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Sandanayaka V, et al. Discovery of 4-[(2S)-2-{[4-(4-chlorophenoxy)phenoxy]methyl}-1-pyrrolidinyl]butanoic acid (DG-051) as a novel leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis. J Med Chem. 2010 Jan 28;53(2):573-85. [Content Brief]
[2]. Enache LA, et al. Synthesis and structural assignment of two major metabolites of the LTA4H inhibitor DG-051. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6275-9. [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 (sealed storage, away from moisture). 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 | 2.3456 mL | 11.7280 mL | 23.4560 mL | 58.6400 mL |
| 5 mM | 0.4691 mL | 2.3456 mL | 4.6912 mL | 11.7280 mL | |
| 10 mM | 0.2346 mL | 1.1728 mL | 2.3456 mL | 5.8640 mL | |
| 15 mM | 0.1564 mL | 0.7819 mL | 1.5637 mL | 3.9093 mL | |
| 20 mM | 0.1173 mL | 0.5864 mL | 1.1728 mL | 2.9320 mL | |
| 25 mM | 0.0938 mL | 0.4691 mL | 0.9382 mL | 2.3456 mL | |
| 30 mM | 0.0782 mL | 0.3909 mL | 0.7819 mL | 1.9547 mL | |
| 40 mM | 0.0586 mL | 0.2932 mL | 0.5864 mL | 1.4660 mL | |
| 50 mM | 0.0469 mL | 0.2346 mL | 0.4691 mL | 1.1728 mL | |
| 60 mM | 0.0391 mL | 0.1955 mL | 0.3909 mL | 0.9773 mL | |
| 80 mM | 0.0293 mL | 0.1466 mL | 0.2932 mL | 0.7330 mL | |
| 100 mM | 0.0235 mL | 0.1173 mL | 0.2346 mL | 0.5864 mL |
DG051 Related Classifications
HY-10825 Related Classifications
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