Lodelaben
Based on 1 Customer Validation
Lodelaben is a human neutrophil elastase inhibitor with an IC50 and Ki of 0.5 and 1.5 μM, respectively.
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- Pureté: 95.0%
- CAS No.: 111149-90-7
- Formule: C25H41ClO3
- Masse moléculaire:425.04
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
Lodelaben is a human neutrophil elastase inhibitor with an IC50 and Ki of 0.5 and 1.5 μM, respectively. Results indicate that the inhibition of human neutrophil elastase (HNE) by Lodelaben is non-competetive. Lodelaben is not inhibitory at 10 μM with the synthetic substrates or at 5 μM vith Azocoll. Pseudomonas aeruginosa elastase, a metallo-protease is not inhibited by Lodelaben. Cathepsin G activity, however, is inhibited by Lodelaben, with an IC50 of approximately 2.5 μM, with Azocoll as substrate[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 111149-90-7
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Appearance Solid
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Masse moléculaire 425.04
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Formule C25H41ClO3
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Color White to off-white
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SMILES
O=C(O)C1=CC=C(C(O)CCCCCCCCCCCCCCCCC)C=C1Cl
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Synonyms
SC-39026; Declaben
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Protocole
Human neutrophil elastase (HNE) activity is quantitated by two assay systems. In the first, the rate of hydrolysis of MeOS-AAPV-NA is monitored spectrophotometrically at 410 nm, in the presence or absence of Lodelaben. The elastase concentration is titrated to yield an absorption change of 0.12 to 0.14 optical density units/min, at 30°C, in 0.2 M Tris buffet, pH 8. Lodelaben and substrate are prepared in dimethylsulfoxide (DHSO). The final DMSO concentration is 10%. In the second method, the hydrolysis of [14C]elelastin by HNE in the presence and absence of Lodelaben is quantitated[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pathogen-free male Sprague-Dawley rats (250 to 300 g) are used. Half are assigned at random to be given a single subcutaneous injection of monocrotaline (60 mg/kg) and the other half receive an equal volume of 0.9% saline. Half of the rats in each group are further assigned at random to receive by gavage either Lodelaben (40 mg/kg/dose) suspended in carboxymethylcellulose vehicle or an equal volume of vehicle only. The rats are gavaged twice daily starting 12 hours before and continuing for 8 days after the monocrotaline or saline injection to provide a "window" around day 4. On day 13, after the monocrotaline or saline injection, the rats are anesthetized. Pressure measurements and cardiac output are recorded 48 hours later to allow sufficient time for recovery from the effects of anesthesia. The heart and lungs are then prepared for morphological assessments[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (268 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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Instruction de manipulation (2659 KB)
Références
[1]. Nakao A, et al. SC-39026, a specific human neutrophil elastase inhibitor. Biochem Biophys Res Commun. 1987 Sep 15;147(2):666-74. [Content Brief]
[2]. Ilkiw R, et al. SC-39026, a serine elastase inhibitor, prevents muscularization of peripheral arteries, suggesting a mechanism of monocrotaline-induced pulmonary hypertension in rats. Circ Res. 1989 Apr;64(4):814-25. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)