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Clarithromycin P450 (e.g. CYP17) inhibitor

Cat.No.S2555

Clarithromycin (A-56268) is a macrolide antibiotic and a CYP3A4 inhibitor, used to treat a number of bacterial infections.
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Quality Control

Batch: Purity: 99.98%
99.98

Solubility

In vitro
Batch:

DMSO : 18 mg/mL (24.06 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 747.95 Formula

C38H69NO13

Storage (From the date of receipt)
CAS No. 81103-11-9 Download SDF Storage of Stock Solutions

Synonyms A-56268 SMILES CCC1C(C(C(C(=O)C(CC(C(C(C(C(C(=O)O1)C)OC2CC(C(C(O2)C)O)(C)OC)C)OC3C(C(CC(O3)C)N(C)C)O)(C)OC)C)C)O)(C)O

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
CYP3A4
In vitro
Clarithromycin suppresses this production in a dose-dependent manner in both monocytes and THP-1 cells. This compound 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). It suppresses NF-kappaB activation induced by TNF-alpha in U-937 and Jurkat cells in a concentration-related manner. The chemical inhibits NF-kappaB activation induced by TNF-alpha in U-937, Jurkat, and A549 cells and PBMC and by SEA in PBMC. It prevents NF-kappaB-dependent reporter gene expression in U-937 cells. This agent results in a significant suppression of production of each cytokine in 71% and a significant increase in 29% of the human monocytes. It inhibits tumor necrosis factor (TNF)-alpha-induced IL-8 gene expression in a dose- and incubation time-dependent manner. This compound represses AP-1 binding in TNF-alpha-treated BET-1A cells. It represses IL-8 gene transcription mainly via the AP-1 binding site in human bronchial epithelial cells. The substance suppresses IL-1 beta gene expression in human nasal epithelial cells stimulated by H. influenzae endotoxin (HIE). It suppresses intercellular adhesion molecule-1 gene expression in nasal fibroblasts stimulated by IL-1 beta. This chemical reduces DNA-binding activity of NF-kappa B in both human nasal epithelial cells and fibroblasts stimulated by HIE or IL-1 beta, respectively.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/10615065/
  • [5] https://pubmed.ncbi.nlm.nih.gov/10646728/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-03-20)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07485010 NOT_YET_RECRUITING
Mycobacterium Abscessus Pulmonary Disease; Mycobacterium Abscessus Infection; Non-Tuberculous Mycobacterial (NTM) Infections; Non-Tuberculous Mycobacteria Pulmonary Disease
The University of Queensland
2027-04 PHASE2
NCT04415983 RECRUITING
Helicobacter Pylori Infection
Tanta University
2020-06-01 PHASE3
NCT04310930 RECRUITING
Pulmonary Disease Due to Mycobacteria (Diagnosis)
The University of Queensland
2020-03-02 PHASE2; PHASE3
NCT07104318 NOT_YET_RECRUITING
Helicobacter Pylori
VA Office of Research and Development
2026-10-01 PHASE3
NCT03236987 RECRUITING
Lung Infection; MAC Lung Disease
Centre Hospitalier Universitaire, Amiens
2018-02-05 PHASE3
NCT07341100 ACTIVE_NOT_RECRUITING
Ovarian Epithelial Cancer
Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd.
2026-01-16 PHASE2

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