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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 95.0%
- CAS 番号: 111149-90-7
- 分子式: C25H41ClO3
- 分子量:425.04
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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.
化学情報
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CAS 番号 111149-90-7
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性状 Solid
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分子量 425.04
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分子式 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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別名
SC-39026; Declaben
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
プロトコル
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.
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)