Nedocromil
Based on 1 Customer Validation
Nedocromil (FPL 59002) is a mast cell stabilizer and an inhibitor of IL-8 production. Nedocromil inhibits mast cell degranulation and collagen synthesis induced by activated mast cells, indirectly interfering with IL-1β signaling. Nedocromil reduces conjunctival eosinophil infiltration and improves the cutaneous manifestations of chronic graft-versus-host disease (including reducing fibrosis, loss of fat and hair follicles, and inflammatory infiltration). Nedocromil can be used in research on chronic graft-versus-host disease, asthma, and allergic conjunctivitis.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.19%
- CAS. Nr.: 69049-73-6
- Formel: C19H17NO7
- Molecular Weight:371.34
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
IL-1β |
IL-8 |
In Vitro
Nedocromil sodium (up to 10-5 mol/L; 8 h) does not directly affect the chemotactic activity of IL-1β-stimulated human bronchial epithelial cell-conditioned media on human neutrophils[2].
Nedocromil sodium (10-5 mol/L; 4 h) significantly and dose-dependently reduces the IL-1β-induced release of immunoreactive IL-8 from cultured human bronchial epithelial cells without affecting constitutive release[2].
Nedocromil sodium (10-5 mol/L; 4 h) prevents the increased expression of IL-8 mRNA induced by IL-1β in cultured human bronchial epithelial cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human neutrophils and human bronchial epithelial cells
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Concentration:up to 10^-5 mol/L
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Incubation Time:8 h
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Result:Did not significantly affect the chemotactic activity of epithelial cell-conditioned media at concentrations up to 10^-5 mol/L.
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Cell Line:Human bronchial epithelial cells
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Concentration:10^-5 mol/L (preincubation); 5 ng/mL (IL-1β)
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Incubation Time:3-5 h (preincubation); 8 h (IL-1β stimulation)
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Result:Reduced the release of immunoreactive IL-8 by >50% when added 3 to 5 hours before IL-1β.
Significantly reduced the release of immunoreactive IL-8 induced by IL-1β in a dose-dependent manner when preincubated for 4 hours.
Did not modify the constitutive release of IL-8 at concentrations up to 10^-5 mol/L.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6-10 weeks, 20-25 g)[1]
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Dosage:5 mg/mouse
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Administration:i.p.; daily; 15 days
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Result:Decreased the mean dermis/fat ratio to 1.5 compared to 4.0 in saline-treated cGVHD mice.
Normalized skin mast cell numbers from 1.71 to 2.95.
Increased peritoneal mast cell numbers to 1.45 compared to 0.25 in controls.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 69049-73-6
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Appearance Solid
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Molecular Weight 371.34
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Formel C19H17NO7
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Color Light yellow to yellow
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SMILES
O=C(C1=CC(C2=CC3=C(N(CC)C(C(O)=O)=CC3=O)C(CCC)=C2O1)=O)O
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Synonyms
FPL 59002
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 16.67 mg/mL (44.89 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (284 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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Handling Instructions (2659 KB)
Verweise
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6929 mL | 13.4647 mL | 26.9295 mL | 67.3237 mL |
| 5 mM | 0.5386 mL | 2.6929 mL | 5.3859 mL | 13.4647 mL | |
| 10 mM | 0.2693 mL | 1.3465 mL | 2.6929 mL | 6.7324 mL | |
| 15 mM | 0.1795 mL | 0.8976 mL | 1.7953 mL | 4.4882 mL | |
| 20 mM | 0.1346 mL | 0.6732 mL | 1.3465 mL | 3.3662 mL | |
| 25 mM | 0.1077 mL | 0.5386 mL | 1.0772 mL | 2.6929 mL | |
| 30 mM | 0.0898 mL | 0.4488 mL | 0.8976 mL | 2.2441 mL | |
| 40 mM | 0.0673 mL | 0.3366 mL | 0.6732 mL | 1.6831 mL |
Keywords
- Nedocromil
- 69049-73-6
- FPL 59002
- FPL59002
- FPL-59002
- Interleukin Related
- IL-1β-induced IL-8 production
- human bronchial epithelial cells
- asthma
- mast cell stabilizer
- skin mast cell numbers
- mast cell degranulation
- IL-8 mRNA
- allergic conjunctivitis
- chronic graft-versus-host disease
- human neutrophils
- Inhibitor
- inhibitor
- inhibit