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Fidaxomicin DNA/RNA Synthesis inhibitor

Cat.No.S4227

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

Batch: Purity: 99.76%
99.76

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (94.51 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% 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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 1058.04 Formula

C52H74Cl2O18

Storage (From the date of receipt)
CAS No. 873857-62-6 Download SDF Storage of Stock Solutions

Synonyms OPT-80, PAR-101 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

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Mechanism of Action

Targets/IC50/Ki
RNA polymerase
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 this compound will inhibit protein synthesis. As a result, apoptosis is triggered in susceptible organisms such as C. difficile.

In vivo

The minimum inhibitory concentration for 90% of organisms for fidaxomicin against C. difficile is 0.9978 to 2 μg/mL. This compound 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 this chemical are much higher and are concentration-dependent. Cmax = 2 hours; Tmax = 5.2 ng/mL; AUC = 14 ng•hr/mL. It 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 this compound.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-11-03)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06794944 NOT_YET_RECRUITING
Inflammatory Bowel Disease (IBD); Clostridioides Difficile Infection
Brigham and Women's Hospital
2026-09 PHASE4
NCT07328971 RECRUITING
Clostridia Difficile Colitis
McGill University Health Centre/Research Institute of the McGill University Health Centre
2026-04-24 PHASE3
NCT05266807 RECRUITING
Clostridioides Difficile Infection
Benoit Guery
2023-03-15 PHASE3
NCT07120490 NOT_YET_RECRUITING
Clostridioides Difficile Infection; Clostridioides Difficile Infection Recurrence; Fecal Microbiota Transplantation (FMT); Comparative Effectiveness of CDI Treatments; Fidaxomicin; Vancomycin
Medical University of Warsaw
2025-10
NCT02667418 TERMINATED
Clostridium; Difficile; Fidaxomicin; Vancomycin
VA Office of Research and Development
2016-02-19 PHASE4
NCT05201079 COMPLETED
Recurrent Clostridium Difficile Infection; Primary Clostridium Difficile Infection
Mikrobiomik Healthcare Company S.L.
2021-10-29 PHASE3

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