Zincov
Zincov is an orally active hydroxamic acid derivative and bacterial metalloproteinase inhibitor. Zincov blocks chloride ion binding by binding to the active site of thermolysin, thereby inhibiting the hydrolysis and blood coagulation reactions catalyzed by this enzyme. Meanwhile, Zincov attenuates cytotoxicity, prevents protein degradation and ZO-1 rearrangement without affecting the functions of other common proteases. Zincov exhibits blood glucose-regulating and antioxidant activities; it reduces blood glucose levels and increases liver dry weight in diabetic rats, but elevates blood glucose levels in normal rats. Zincov is widely used in studies related to cholera and diabetes.
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。
- CAS 番号: 71431-46-4
- 分子式: C12H22N4O5
- 分子量:302.33
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
Zincov (0-800 nM; 1 h) inhibits thermolysin-catalyzed FAGLA hydrolysis with a Ki of 180 nM at pH 7.5 and 25°C[1].
Zincov (500 μM; 30 min-3.5 h) potently attenuates HA/P-mediated degradation of occludin in MDCK-I cells[3].
Zincov (500 μM; 15 min) prevents HA/P-mediated rearrangement of ZO-1 in MDCK-I cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mardin-Darby canine kidney epithelial cell line I (MDCK-I) cells
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Concentration:500 μM
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Incubation Time:30 min; 1 h; 2 h; 3.5 h
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Result:Greatly attenuated the HA/P-mediated degradation of occludin (66-85 kDa) into 50 kDa and 35 kDa fragments, as shown by preservation of the full-length occludin bands and reduction in the intensity of the degradation product bands.
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Cell Line:Mardin-Darby canine kidney epithelial cell line I (MDCK-I) cells
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Concentration:500 μM
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Incubation Time:15 min
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Result:Prevented the HA/P-mediated rearrangement of ZO-1, maintaining ZO-1 as narrow continuous ribbons along cell-cell boundaries, similar to untreated cells.
化学情報
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CAS 番号 71431-46-4
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分子量 302.33
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分子式 C12H22N4O5
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SMILES
NC(CNC([C@H](C)NC(C(CC(C)C)C(NO)=O)=O)=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Inouye K, et al. A spectrophotometric study on the interaction of thermolysin with chloride and bromide ions, and the state of tryptophyl residue 115. J Biochem. 1994;116(3):530-535. [Content Brief]
[2]. Booth BA, et al. Vibrio cholerae soluble hemagglutinin/protease is a metalloenzyme. Infect Immun. 1983;42(2):639-644. [Content Brief]
[3]. Wu Z, et al. Distinct effects of Vibrio cholerae haemagglutinin/protease on the structure and localization of the tight junction-associated proteins occludin and ZO-1. Cell Microbiol. 2000;2(1):11-17. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)