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抑制剂描述:

产品名称:Clarithromycin

产品别名:见爱必信官网

英文别名:Clarithromycin

靶点:P450

CAS:81103-11-9

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Clarithromycin (Biaxin, Klacid) is a macrolide antibiotic and a CYP3A4 substrate and inhibitor. Clarithromycin (Biaxin, Klacid) prevents bacteria from growing by interfering with their protein synthesis. Clarithromycin (Biaxin, Klacid) binds to the subunit 50S of the bacterial ribosome and thus inhibits the translation of peptides. Clarithromycin (Biaxin, Klacid) has similar antimicrobial spectrum as erythromycin but is more effective against certain gram-negative bacteria, particularly Legionella pneumophila. Clarithromycin (Biaxin, Klacid) is used to treat pharyngitis, tonsillitis, acute maxillary sinusitis, acute bacterial exacerbation of chronic bronchitis, pneumonia (especially atypical pneumonias associated with Chlamydia pneumoniae or TWAR), skin and skin structure infections. Besides, clarithromycin (Biaxin, Klacid)is a substrate and inhibitor of CYP3A4. Inhibitors of CYP3A4 may increase clarithromycin (Biaxin, Klacid) serum concentrations. Inducers of CYP3A4 substrates may decrease clarithromycin (Biaxin, Klacid) serum concentrations.

溶解性:DMSO :25 mg/mL warmed (33.4 mM)

体外研究:

Clarithromycin suppresses this production in a dose-dependent manner in both monocytes and THP-1 cells. Clarithromycin regulates three other promoters that have either the NF-kappa B or the AP-1 binding sequences: two synthetic (pAP-1-Luc and pNF-kappa B-Luc) and one naturally occurring (ELAM-Luc). Clarithromycin suppresses NF-kappaB activation induced by TNF-alpha in U-937 and Jurkat cells in a concentration-related manner. Clarithromycin inhibits NF-kappaB activation induced by TNF-alpha in U-937, Jurkat, and A549 cells and PBMC and by SEA in PBMC. Clarithromycin prevents NF-kappaB-dependent reporter gene expression in U-937 cells. Clarithromycin results in a significant suppression of production of each cytokine in 71% and a significant increase in 29% of the human monocytes. Clarithromycin inhibits tumor necrosis factor (TNF)-alpha-induced IL-8 gene expression in a dose- and incubation time-dependent manner. Clarithromycin represses AP-1 binding in TNF-alpha-treated BET-1A cells. Clarithromycin represses IL-8 gene transcription mainly via the AP-1 binding site in human bronchial epithelial cells. Clarithromycin suppresses IL-1 beta gene expression in human nasal epithelial cells stimulated by H. influenzae endotoxin (HIE). Clarithromycin suppresses intercellular adhesion molecule-1 gene expression in nasal fibroblasts stimulated by IL-1 beta. Clarithromycin reduces DNA-binding activity of NF-kappa B in both human nasal epithelial cells and fibroblasts stimulated by HIE or IL-1 beta, respectively.

体内研究:

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