Fidaxomicin

製品コードS4227 バッチS422710

印刷

化学情報

Synonyms

OPT-80, PAR-101

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₅₂H₇₄Cl₂O₁₈

分子量

1058.04

CAS No.

873857-62-6

Solubility (25°C)*

体外

DMSO

100 mg/mL (94.51 mM)

Ethanol

25 mg/mL (23.62 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution	5% DMSO 1 95% Corn oil	0.5mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Fidaxomicin is a narrow spectrum macrocyclic antibiotic that inhibits RNA polymerase sigma subunit.
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]

プロトコル(参考用のみ)

参考

[1] Venugopal AA, et al. Clin Infect Dis, 2012, 54(4), 568-574.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。