生物活性 | |||
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描述 | Meticrane is a diuretic and a potent peripheral-type benzodiazepine receptor (PBR) inhibitor (IC50= 1 μM). Meticrane inhibits the reabsorption of sodium and chloride ions in the distal convoluted tubule. Meticrane is used to treat essential hypertension[3]. Meticrane is highly ranked in the connectivity map (cMap) analysis, and it does not have any known anti-cancer or immune-stimulating effect. Co-treatment with Meticrane significantly enhances treatment efficacy of CTLA-4 blockade[4]. In vitro assays performed in presence of 6-hydroxycoumarin and meticrane, among the highly affinity predicted binders, confirmed a dose-dependent inhibition (17-81%) of patulin production by 6-hydroxycoumarin (10 µM-1 mM concentration range), whereas the approved drug meticrane inhibited patulin production by 43% already at 10 µM. Furthermore, 6-hydroxycoumarin and meticrane caused a 60 and 41% reduction of patulin production, respectively, in vivo on apples at 100 µg/wound[5]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.63mL 0.73mL 0.36mL |
18.16mL 3.63mL 1.82mL |
36.32mL 7.26mL 3.63mL |
参考文献 |
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