Clarithromycin

Catalog No.S2555 Synonyms: A-56268

Clarithromycin  Chemical Structure

Molecular Weight(MW): 747.95

Clarithromycin is a macrolide antibiotic and a CYP3A4 inhibitor, used to treat a number of bacterial infections.

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Biological Activity

Description Clarithromycin is a macrolide antibiotic and a CYP3A4 inhibitor, used to treat a number of bacterial infections.
Targets
CYP3A4 [1]
In vitro

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). [1] 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. [2] Clarithromycin results in a significant suppression of production of each cytokine in 71% and a significant increase in 29% of the human monocytes. [3] 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. [4] 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. [5]

Protocol

Solubility (25°C)

In vitro DMSO 25 mg/mL warmed (33.42 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 747.95
Formula

C38H69NO13

CAS No. 81103-11-9
Storage powder
in solvent
Synonyms A-56268

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03800550 Completed Drug: Bedaquiline|Drug: Clarithromycin Healthy Janssen Research & Development LLC February 13 2019 Phase 1
NCT03043989 Terminated Drug: Docetaxel|Drug: Cabazitaxel|Drug: Clarithromycin Prostate Cancer Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Maryland Technology Development Corporation March 21 2017 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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P450 (e.g. CYP17) Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID