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Azithromycin Antibiotics for Mammalian Cell Culture inhibitor

Cat.No.S1835

Azithromycin is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections.
Azithromycin Antibiotics for Mammalian Cell Culture inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 748.98

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Quality Control

Batch: Purity: >97%
97

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa 299 Antichlamydial assay 44 to 48 hrs Antichlamydial activity against Chlamydia trachomatis serovar L2 infected in human HeLa 299 cells assessed as reduction in number of inclusion bodies measured after 44 to 48 hrs by DAPI staining-based HCS assay, IC50=0.727μM. 29232584
THP1 Function assay 30 mins Drug uptake in human THP1 cells at pH 6 to 7 after 30 mins 19564365
THP1 Function assay 24 hrs Drug uptake in human THP1 cells after 24 hrs in presence of verapamil 19564365
THP1 Function assay 24 hrs Drug uptake in human THP1 cells after 24 hrs in presence of gemfibrozil 19564365
Hep2 Antichlamydial assay 4 ug/ml 8 hrs Anti-Chlamydial activity against Chlamydia trachomatis Serovar LGV-L2 infected in Hep2 cells assessed as reduction in size and number of chlamydial inclusion at 4 ug/ml treated at 8 hrs post-infection and 24 hrs later re-infecting fresh Hep2 cells monolay 32227948
Vero E6 Antiviral assay 2 days Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days, EC50=2.12μM. ChEMBL
Vero E6 Antiviral assay 2 days Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days, EC90=8.65μM. ChEMBL
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Solubility

In vitro
Batch:

DMSO : 100 mg/mL (133.51 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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% ddH2O
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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
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Chemical Information, Storage & Stability

Molecular Weight 748.98 Formula

C38H72N2O12

 Storage (From the date of receipt)
CAS No. 83905-01-5 Download SDF Storage of Stock Solutions

Synonyms XZ-450,CP-62993 Smiles CCC1C(C(C(N(CC(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)O)C)C)C)O)(C)O

Mechanism of Action

Targets/IC50/Ki
protein synthesis
In vitro
Azithromycin reduces about 40% of IL-8 mRNA and protein expression in cystic fibrosis (CF) cells reaching the levels of non-CF cells. This compound results in 50% and 70% reduction of NF-kappaB and AP-1 DNA binding, respectively, leading to levels of non-CF cells. It significantly enhances the intensity of a co-stimulatory molecule, CD80, on DCs but not CD86 and CD40 in dendritic cells (DCs). This macrolide significantly increases the production of IL-10 and Clarithromycin (CAM) significantly inhibits the production of IL-6 by DCs. It increases IL-10 and CAM decreases IL-2 productions significantly, when naive T cells derived from spleen are co-cultured with DCs treated in advance with LPS and these macrolides. This agent selectively inhibits fluid-phase endocytosis of horseradish peroxidase and lucifer yellow in J774 mouse macrophages. It delays sequestration of receptor-bound transferrin and peroxidase-anti-peroxidase immune complexes into cell-surface endocytic pits and vesicles. This chemical down-regulates cell surface transferrin receptors, but not Fc gamma receptors, by causing a major delay in the accessibility of internalized transferrin receptors to the recycling route, without slowing down subsequent efflux, resulting in redistribution of the surface pool to an intracellular pool. It inserts into the DOPC lipid bilayer, so as to decrease its cohesion and to facilitate the merging of DPPC into the DOPC fluid matrix.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/17537401/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05972772 Not yet recruiting
Infectious Disease|Therapeutics
Lao-Oxford-Mahosot Hospital Wellcome Trust Research Unit|Mahidol Oxford Tropical Medicine Research Unit
 March 20 2024 Phase 2|Phase 3
NCT05796362 Not yet recruiting
Infectious Disease|Drug Effect|Clinical Infection
Brigham and Women''s Hospital|Bill and Melinda Gates Foundation
 April 2023 Phase 1

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