Clarithromycin

SKU: orb1308632

Description

Clarithromycin (A-56268) is a macrolide antibiotic that acts by inhibiting bacterial protein synthesis. It is also a known inhibitor of cytochrome P450 3A4 and P-glycoprotein, making it a useful pharmacological tool for studying drug metabolism, transport, and bacterial resistance in both in vitro and in vivo research models.

Research Area

Cell Biology, Immunology & Inflammation, Infectious Disease & Virology, Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 81103-11-9
• MW: 747.95
• Purity: 99.89% (May vary between batches)
• Formula: C₃₈H₆₉NO₁₃
• SMILES: O([C@H]1[C@@](OC)(C)C[C@@H](C)C(=O)[C@H](C)[C@@H](O)[C@](C)(O)[C@@H](CC)OC(=O)[C@H](C)[C@@H](O[C@H]2C[C@](OC)(C)[C@@H](O)[C@H](C)O2)[C@@H]1C)[C@H]3[C@H](O)[C@@H](N(C)C)C[C@@H](C)O3
• Target: Cytochromes P450,Autophagy,Antibacterial,MRP,Antibiotic,ribosome
• Solubility: DMSO:38 mg/mL (50.81 mM);10% DMSO+90% Corn Oil:2 mg/mL (2.67 mM)

Bioactivity

• 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). 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HERG, flux, Inhibitor, inhibit, MRP1, Cytochrome P450, CYPs, CYP3A4, current, Clarithromycin, autophagic, Autophagy, Bacterial, Antibiotic, Antimicrobial, A 56268, A56268, A-56268, 50S ribosome, potassium

Compound Identifiers

PubChem CID

84029