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Formula | C52H74Cl2O18 |
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Molecular Weight | 1058.04 | CAS No. | 873857-62-6 | |
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (94.51 mM) | |
Ethanol | 25 mg/mL (23.62 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.) |
Description | Fidaxomicin is a narrow spectrum macrocyclic antibiotic that inhibits RNA polymerase sigma subunit. | |
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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] |
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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] |
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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