Freselestat
Based on 1 Customer Validation
Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity.
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- Pureté : 99.00%
- CAS No.: 208848-19-5
- Formule: C23H28N6O4
- Masse moléculaire:452.51
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Stockage:Powder -20°C, 3 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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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HY-111457A
BAY-678 -
HY-17443A
Sivelestat sodium -
HY-17443
SivelestatElastase Inhibitor -
HY-15651
AlvelestatNeutrophil Elastase Inhibitor -
HY-17443B
Sivelestat sodium tetrahydrateNeutrophil Elastase Inhibitor -
HY-75957
DMP 777Elastase Inhibitor -
HY-15891A
GW311616 hydrochlorideHNE Inhibitor -
HY-19908
BAY-85-8501HNE Inhibitor -
HY-15891
GW311616HNE Inhibitor -
HY-17443BR
Sivelestat sodium tetrahydrate (Standard)Neutrophil Elastase Inhibitor -
HY-17443R
Sivelestat (Standard)Elastase Inhibitor -
HY-100397
ElastatinalElastase Inhibitor
Activité biologique
Description
IC50 & Target
Ki: 12.2 nM (Neutrophil elastase)[3]
In Vitro
Simulated extracorporeal circulation is established by recirculating fresh heparinized (3.75 U/mL) human blood for 120 minutes in a membrane oxygenator and a roller pump with and without 1.0 μM of Freselestat (ONO-6818). Neutrophil elastase levels are significantly lower in the Freselestat group. Freselestat significantly reduces interleukin 8 and C5b-9 production. Freselestat does not modulate changes of CD11b and L-selectin during recirculation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 Wistar rats (228 g) induced by human neutrophil elastase (HNE)[1]
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Dosage:10 mg/kg, 100 mg/kg
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Administration:Oral administration; daily; for 8 weeks
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Result:Attenuated dose-dependently HNE-induced increases in lung myeloperoxidase activity, hemoglobin, and neutrophil count in bronchoalveolar lavage fluid.
Chemical Information
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CAS No. 208848-19-5
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Appearance Solid
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Masse moléculaire 452.51
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Formule C23H28N6O4
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Color White to off-white
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SMILES
O=C(NC(C(C1=NN=C(C(C)(C)C)O1)=O)C(C)C)CN(C(C2=CC=CC=C2)=NC=C3N)C3=O
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Synonyms
ONO-6818; ONO-PO-736
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (220.99 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)
Pureté et documentation
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Fiche technique (276 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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Instruction de manipulation (2659 KB)
Références
[1]. Am J Respir Crit Care Med. 2002 Aug 15;166(4):496-500. [Content Brief]
[2]. K Ohmoto, et al. Design and synthesis of new orally active inhibitors of human neutrophil elastase. Bioorg Med Chem. 2001 May;9(5):1307-23. [Content Brief]
[3]. Yasushi Hirota, et al. Effects of the neutrophil elastase inhibitor (ONO-6818) on acetic acid induced colitis in Syrian hamsters. J Vet Med Sci. 2004 Oct;66(10):1223-8. [Content Brief]
[4]. Yukihiro Yoshimura, et al. ONO-6818, a novel, potent neutrophil elastase inhibitor, reduces inflammatory mediators during simulated extracorporeal circulation. Ann Thorac Surg. 2003 Oct;76(4):1234-9. [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. 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 | 2.2099 mL | 11.0495 mL | 22.0990 mL | 55.2474 mL |
| 5 mM | 0.4420 mL | 2.2099 mL | 4.4198 mL | 11.0495 mL | |
| 10 mM | 0.2210 mL | 1.1049 mL | 2.2099 mL | 5.5247 mL | |
| 15 mM | 0.1473 mL | 0.7366 mL | 1.4733 mL | 3.6832 mL | |
| 20 mM | 0.1105 mL | 0.5525 mL | 1.1049 mL | 2.7624 mL | |
| 25 mM | 0.0884 mL | 0.4420 mL | 0.8840 mL | 2.2099 mL | |
| 30 mM | 0.0737 mL | 0.3683 mL | 0.7366 mL | 1.8416 mL | |
| 40 mM | 0.0552 mL | 0.2762 mL | 0.5525 mL | 1.3812 mL | |
| 50 mM | 0.0442 mL | 0.2210 mL | 0.4420 mL | 1.1049 mL | |
| 60 mM | 0.0368 mL | 0.1842 mL | 0.3683 mL | 0.9208 mL | |
| 80 mM | 0.0276 mL | 0.1381 mL | 0.2762 mL | 0.6906 mL | |
| 100 mM | 0.0221 mL | 0.1105 mL | 0.2210 mL | 0.5525 mL |
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