Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor Fidaxomicin For research use only.

Fidaxomicin

Synonyms: OPT-80, PAR-101

Fidaxomicin is a narrow spectrum macrocyclic antibiotic that inhibits RNA polymerase sigma subunit.

Fidaxomicin Chemical Structure

Fidaxomicin Chemical Structure

CAS: 873857-62-6

Selleck's Fidaxomicin has been cited by 8 publications

Purity & Quality Control

Batch: Purity: 99.76%
99.76

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Biological Activity

Description Fidaxomicin is a narrow spectrum macrocyclic antibiotic that inhibits RNA polymerase sigma subunit.
Targets
RNA polymerase [1]
In vitro
In vitro

Fidaxomicin acts as a RNA polymerase inhibitor by binding to the DNA template–RNA polymerase (RNAP) complex prior to the formation of the open RNAP-DNA complex in which transcription is initiated. Therefore it will inhibit protein synthesis. As a result, apoptosis is triggered in susceptible organisms such as C. difficile. [1]
In Vivo
In vivo

The minimum inhibitory concentration for 90% of organisms for fidaxomicin against C. difficile is 0.9978 to 2 μg/mL. Fidaxomicin is not systemically absorbed as shown by a plasma concentrations below the lower limit of quantification after single-dose or multiple-dose. In contrast, fecal concentrations of fidaxomicin are much higher and are concentration-dependent. Cmax = 2 hours; Tmax = 5.2 ng/mL; AUC = 14 ng•hr/mL. Fidaxomicin is hydrolyzed by gastric acid or intestinal microsomes into a less active metabolite (OP-1118). The cytochrome enzyme system are not involved in the metabolism of fidaxomicin. [1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04138706 Recruiting Clostridium Difficile Infection McGill University Health Centre/Research Institute of the McGill University Health Centre|Canadian Institutes of Health Research (CIHR) November 19 2020 Phase 3
NCT02437591 Completed Inflammatory Bowel Disease (IBD)|Clostridium Difficile Infection (CDI) Astellas Pharma Europe Ltd.|Astellas Pharma Inc August 13 2015 Phase 4
NCT02395848 Terminated Clostridium Difficile Infection McMaster University July 2015 Phase 3

Chemical lnformation & Solubility

Molecular Weight 1058.04 Formula

C52H74Cl2O18
CAS No. 873857-62-6 SDF Download Fidaxomicin SDF
Smiles CCC1C=C(C(CC=CC=C(C(=O)OC(CC=C(C=C(C1OC2C(C(C(C(O2)(C)C)OC(=O)C(C)C)O)O)C)C)C(C)O)COC3C(C(C(C(O3)C)OC(=O)C4=C(C(=C(C(=C4O)Cl)O)Cl)CC)O)OC)O)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (94.51 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble


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In vivo
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In vivo Formulation Calculator

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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.

Tech Support

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.

Handling Instructions

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