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Clarithromycin

CAS No. : 81103-11-9

MCE 国际站：Clarithromycin

产品活性：Clarithromycin 具有广谱的抗菌 (antimicrobial) 活性。Clarithromycin 抑制 CYP3A4 催化的三唑仑 α-羟基化，IC₅₀ (K_i) 值为 56 (43) μM。Clarithromycin 抑制 HERG 钾电流。Clarithromycin 通过削弱连接 hERG1 和 PI3K 的信号通路来影响自噬流 (autophagic flux)。

研究领域：Anti-infection  |  Metabolic Enzyme/Protease  |  Autophagy

作用靶点：Bacterial  |  Cytochrome P450  |  Autophagy  |  Antibiotic

In Vitro: Clarithromycin produces a similar concentration-dependent block with an IC₅₀ of 45.7 µM.
Clarithromycin induces the formation of numerous intracytoplasmic vacuoles after 24 h, in all cell lines, especially in HCT116 cells. Prolonged treatment with Clarithromycin (40, 80, and 160 µM) alters cell proliferation and triggers apoptotic cell death in colorectal cancer (CRC) cells. Inhibition of cell proliferation is potentiated when Clarithromycin is re-added to the cells. In particular, 160 μM Clarithromycin, re-added after 48 h of incubation, produces an arrest of cell proliferation at 72 h. Similar effects are obtained in LS174T cells.
Clarithromycin (80 and 160 µM; 48 hours) strongly increases the LC3-II/LC3-I ratio, in a dose- and time-dependent manner, with a maximum at 24 h of treatment. This effect is accompanied by a decrease of p62/SQSTM1.

In Vivo: Clarithromycin at 200 mg/kg has activity against four tested in vivo.

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