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  2. Metabolic Enzyme/Protease
  3. Elastase
  4. Lodelaben

Lodelaben 是一種人類嗜中性粒細(xì)胞彈性蛋白酶抑制劑，其 IC50 和 Ki 值分別 0.5 和 1.5 μM。

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Lodelaben

Lodelaben Chemical Structure

CAS No. : 111149-90-7

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規(guī)格 價格 是否有貨 數(shù)量
1 mg ￥2380
In-stock
5 mg ￥5910
In-stock
10 mg   詢價  
50 mg   詢價  

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Customer Review

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Lodelaben is a human neutrophil elastase inhibitor with an IC50 and Ki of 0.5 and 1.5 μM, respectively.

IC50 & Target

IC50: 0.5 μM (elastase)[1]
Ki: 1.5 μM (elastase)[1]
體外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

The mean pulmonary artery pressures of the saline/vehicle and saline/Lodelaben groups are similar, 16.4±1.1 and 17.4±0.9 mm Hg, respectively. Although, mean pulmonary artery pressure in the monocrotaline/vehicle group is 27.5±0.8 mm Hg, treatment of monocrotaline rats with Lodelaben results in significantly lower values (21.00±1.6 mm Hg, p<0.05). Saline/vehicle and saline/Lodelaben rats have only a small percentage of arteries muscularized at the alveolar wall level (1.9±1.4 and 0.4±0.4%, respectively). Treatment of monocrotaline-injected rats with Lodelaben results in a decreased percentage of alveolar wall arteries muscularized (10.0±3.6%)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

425.04

Formula

C25H41ClO3
CAS 號
性狀

固體

顏色

White to off-white

中文名稱

氯德拉苯
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
純度 & 產(chǎn)品資料

純度: 95.0%

參考文獻(xiàn)
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

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產(chǎn)品名稱：
Lodelaben
目錄號：
HY-100240
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