Fidaxomicin

Catalog No.S4227 Batch:S422706

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Technical Data

Formula

C52H74Cl2O18

Molecular Weight 1058.04 CAS No. 873857-62-6
Solubility (25°C)* In vitro DMSO 100 mg/mL (94.51 mM)
Ethanol 31 mg/mL (29.29 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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

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]

Protocol (from reference)

Selleck's Fidaxomicin has been cited by 9 publications

Genetic determinants of resistance to antimicrobial therapeutics are rare in publicly available Clostridioides difficile genome sequences [ J Antimicrob Chemother, 2024, dkae101] PubMed: 38598696
High-throughput, fluorescent-aptamer-based measurements of steady-state transcription rates for the Mycobacterium tuberculosis RNA polymerase [ Nucleic Acids Res, 2023, 51(19):e99] PubMed: 37739412
High-throughput, fluorescent-aptamer-based measurements of steady-state transcription rates for Mycobacterium tuberculosis RNA polymerase [ bioRxiv, 2023, 2023.03.13.532464] PubMed: 36993414
Molecular dissection of RbpA-mediated regulation of fidaxomicin sensitivity in mycobacteria [ J Biol Chem, 2022, 298(4):101752] PubMed: 35189142
Myxopyronin B inhibits growth of a Fidaxomicin-resistant Clostridioides difficile isolate and interferes with toxin synthesis [ Gut Pathog, 2022, 14(1):4] PubMed: 34991700
Clostridium butyricum enhances colonization resistance against Clostridioides difficile by metabolic and immune modulation [ Sci Rep, 2021, 11(1):15007] PubMed: 34294848
Drug Repurposing of Pyrimidine Analogs as Potent Antiviral Compounds Against Human Enterovirus A71 Infection With Potential Clinical Applications [ Sci Rep, 2020, 18;10(1):8159] PubMed: 32424333
Antibacterial activity of novel dual bacterial DNA type II topoisomerase inhibitors. [ PLoS One, 2020, 15(2):e0228509] PubMed: 32074119
Antiviral candidates against the hepatitis E virus (HEV) and their combinations inhibit HEV growth in in vitro. [ Antiviral Res, 2019, 170:104570] PubMed: 31362004

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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