Fidaxomicin (Synonyms: Clostomicin B1, Lipiarmycin, OPT-80, PAR-101, Tiacumicin B) |
| رقم الكتالوجGC12940 |
فيداكسوميسين (OPT-80) ، مضاد حيوي كبير الحلقات ، هو مثبط فعال وفعال لبوليميراز الحمض النووي الريبي عن طريق الفم
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 873857-62-6
Sample solution is provided at 25 µL, 10mM.
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Fidaxomicin is a macrocyclic antibiotic that inhibits RNA polymerase sigma subunit [1].
Antibiotics are a type of antimicrobial used in the treatment of bacterial infection. They can inhibit the growth of bacteria. Bacterial RNA polymerase mediates RNA synthesis.
Fidaxomicin is a narrow spectrum antibiotic that inhibits RNA polymerase sigma subunit. Fidaxomicin was a macrocyclic-lactone antibiotic produced by Actinomycete species. Fidaxomicin inhibited RNA polymerase in Clostridium difficile [1].
In patients infected with Clostridium difficile, fidaxomicin exhibited a higher clinical cure rate and a lower recurrence rate. In rats, fidaxomicin was safe by the intravenous route and exhibited LD50 value of 200 mg/kg. Fidaxomicin for the treament of Clostridium difficile infection (CDI) had entered Phase III trials [2]. In patients with CDI, fidaxomicin exhibited a lower reappearance of toxin in fecal filtrates and inhibited recurrence of CDI. Also, fidaxomicin preserved the intestinal microbiome during the treatment of CDI [3].
References:
[1]. Srivastava A, Talaue M, Liu S, et al. New target for inhibition of bacterial RNA polymerase: 'switch region'. Curr Opin Microbiol, 2011, 14(5): 532-543.
[2]. Poxton IR. Fidaxomicin: a new macrocyclic, RNA polymerase-inhibiting antibiotic for the treatment of Clostridium difficile infections. Future Microbiol, 2010, 5(4): 539-548.
[3]. Louie TJ, Cannon K, Byrne B, et al. Fidaxomicin preserves the intestinal microbiome during and after treatment of Clostridium difficile infection (CDI) and reduces both toxin reexpression and recurrence of CDI. Clin Infect Dis, 2012, 55 Suppl 2: S132-S142.
| Cell experiment: | |
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Cell lines |
Human colonic fibroblasts |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
20 μM for 6 h; |
|
Applications |
Fidaxomicin (20 μM) prevented toxin A-induced cell rounding in human colonic CCD-18Co fibroblasts [1]. Moreover, Fidaxomicin suppressed toxin production in Clostridium difficile [2]. |
| Animal experiment: | |
|
Animal models |
Male C57BL/6 mice model |
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Dosage form |
5 to 20 μM |
|
Applications |
Treatment with fidaxomicin (20 μM) significantly inhibited toxin A-mediated histologic damage and reduced the mean histology score and ileal IL-1β protein and mRNA expression in the mouse ileum [1]. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: 1. Koon, H. W., Ho, S., Hing, T. C., Cheng, M., Chen, X., Ichikawa, Y., Kelly, C. P. and Pothoulakis, C. (2014) Fidaxomicin inhibits Clostridium difficile toxin A-mediated enteritis in the mouse ileum. Antimicrob Agents Chemother. 58, 4642-4650 2. Babakhani, F., Bouillaut, L., Sears, P., Sims, C., Gomez, A. and Sonenshein, A. L. (2013) Fidaxomicin inhibits toxin production in Clostridium difficile. J Antimicrob Chemother. 68, 515-522 | |
| Cas No. | 873857-62-6 | SDF | |
| المرادفات | Clostomicin B1, Lipiarmycin, OPT-80, PAR-101, Tiacumicin B | ||
| Canonical 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 | ||
| Formula | C52H74Cl2O18 | M.Wt | 1058.04 |
| الذوبان | ≥ 35.27mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.9451 mL | 4.7257 mL | 9.4514 mL |
| 5 mM | 0.189 mL | 0.9451 mL | 1.8903 mL |
| 10 mM | 0.0945 mL | 0.4726 mL | 0.9451 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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.)
Calculation results:
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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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