产品
编 号:F467069
分子式:C38H69NO13
分子量:747.95
产品类型
结构图
CAS No: 81103-11-9
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产品详情
生物活性:
Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM. Clarithromycin significantly inhibits the HERG potassium current.Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K.
体内研究:
Clarithromycin at 200 mg/kg has activity against four tested in vivo.Animal Model:Six-week-old beige(C57BL/6J bgj/bgj) mice which had been infected with viable M. avium ATCC 49601
Dosage:50, 100, 200, or 300 mg/kg
Administration:Administered daily by gavage
Result:Reduced organ cell counts compared with those in mice given no treatment at all doses.Had activity against three additional MAC isolates (MICs for the isolates ranged from 1 to 4 μg/mL by broth dilution) at 200 mg/kg.
体外研究:
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.