Fidaxomicin
(Synonyms: 非达霉素; OPT-80; PAR-101) 目录号 : GC12940
A natural antibiotic
Cas No.:873857-62-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| 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: | |
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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 | |
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.
| Cas No. | 873857-62-6 | SDF | |
| 别名 | 非达霉素; OPT-80; PAR-101 | ||
| 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 | ||
| 分子式 | C52H74Cl2O18 | 分子量 | 1058.04 |
| 溶解度 | ≥ 35.27mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。