Freselestat quarterhydrate
Based on 1 Customer Validation
Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate 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 quarterhydrate has a potent anti-inflammatory activity.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.0%
- Formule: C23H28N6O4.1/4H2O
- Masse moléculaire:457.03
-
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]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
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.
-
Animal Model:Male Wistar rats (228 g) induced by human neutrophil elastase (HNE)[1]
-
Dosage:10 mg/kg, 100 mg/kg
-
Administration:Oral administration; daily; for 8 weeks
-
Result:Attenuated dose-dependently HNE-induced increases in lung myeloperoxidase activity, hemoglobin, and neutrophil count in bronchoalveolar lavage fluid.
Chemical Information
-
Appearance Solid
-
Masse moléculaire 457.03
-
Formule C23H28N6O4.1/4H2O
-
Color White to off-white
-
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.[1/4].O
-
Synonyms
ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 40 mg/mL (87.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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
-
Fiche technique (278 KB)
-
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)
-
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 | 2.1880 mL | 10.9402 mL | 21.8804 mL | 54.7010 mL |
| 5 mM | 0.4376 mL | 2.1880 mL | 4.3761 mL | 10.9402 mL | |
| 10 mM | 0.2188 mL | 1.0940 mL | 2.1880 mL | 5.4701 mL | |
| 15 mM | 0.1459 mL | 0.7293 mL | 1.4587 mL | 3.6467 mL | |
| 20 mM | 0.1094 mL | 0.5470 mL | 1.0940 mL | 2.7351 mL | |
| 25 mM | 0.0875 mL | 0.4376 mL | 0.8752 mL | 2.1880 mL | |
| 30 mM | 0.0729 mL | 0.3647 mL | 0.7293 mL | 1.8234 mL | |
| 40 mM | 0.0547 mL | 0.2735 mL | 0.5470 mL | 1.3675 mL | |
| 50 mM | 0.0438 mL | 0.2188 mL | 0.4376 mL | 1.0940 mL | |
| 60 mM | 0.0365 mL | 0.1823 mL | 0.3647 mL | 0.9117 mL | |
| 80 mM | 0.0274 mL | 0.1368 mL | 0.2735 mL | 0.6838 mL |
Freselestat quarterhydrate Related Classifications
HY-15652A Related Classifications
Powered by Bioz