生物活性 | |||
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描述 | (2-Chloropyridin-4-yl)methanamine hydrochloride is an inhibitor of LOXL2 with an IC50 value of 126 nM, showing greater selectivity for LOXL2 over LOX and three other amine oxidases (MAO-A, MAO-B, and SSAO). In human whole blood assays for LOXL2, the IC50 of (2-Chloropyridin-4-yl)methanamine hydrochloride is 1.45 µM, compared to 126 nM in the absence of blood proteins. Its selectivity for LOXL2+BSA (IC50=190 nM) is 31 times greater than for LOX+BSA (IC50=5.91 µM). (2-Chloropyridin-4-yl)methanamine hydrochloride is inactive against a set of LTQ-free AO enzymes (MAO-A, MAO-B, and SSAO) at 30 µM. It also inhibits three different CYP enzymes (CYP 3A4, 2C9, and 2D6), with IC50 values all above 30 µM[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
5.59mL 1.12mL 0.56mL |
27.93mL 5.59mL 2.79mL |
55.85mL 11.17mL 5.59mL |
参考文献 |
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