Rifabutin
(Synonyms: 利福布丁; Ansamycin; LM-427) 目录号 : GC15046
A rifamycin antibiotic
Cas No.:72559-06-9
Sample solution is provided at 25 µL, 10mM.
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Rifabutin is a naphthalenic ansamycin that derives from rifamycin S and has the activity to against mycobacteria infection with MICs ranged from 0.125 to 0.25 µg/ml [1].
TB (tuberculosis) is a chronic infectious disease caused by Mycobacterium tuberculosis infection. TB can invade to human organs whole body, but mainly affects the lung which is called pulmonary tuberculosis. About 2 billion people has been infected with TB all around the word and the emergence of new infected TB patients is about 8-10 million every year. Rifabutin is an anti-TB medicine used to treat TB infected patients with fewer side effects [1].
Rifabutin is a potent antimycobacterial medicine and has lower toxic than rifampicin. When tested with the mimic human-bacterial plasma membranes, Rifabutin showed high affinity for the bacterial membrane mediated by electrostatic interactions with the phospholipid head groups [2]. In patients with organ transplant, Rifabutin was an excellent medicine to reduce the incidence of TB (tuberculosis) infection [3]. When tested 34 isolates of clinical drug resistant M.tuberculosis with Rifabutin, they showed sensitive to Rifabutin compared with rifampicin treatment [1].
In mice model with TB infected, intravenous administration of Rifabutin reduced bacterial loads in spleen, liver and lung [4].
References:
[1]. Pham, D.D., E. Fattal, and N. Tsapis, Pulmonary drug delivery systems for tuberculosis treatment. Int J Pharm, 2014. 478(2): p. 517-529.
[2]. Pinheiro, M., et al., Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects. J Med Chem, 2013. 56(2): p. 417-26.
[3]. Tabarsi, P., et al., Mycobacterial infection and the impact of rifabutin treatment in organ transplant recipients: A single-center study. Saudi J Kidney Dis Transpl, 2015. 26(1): p. 6-11.
[4]. Gaspar, M.M., et al., Rifabutin encapsulated in liposomes exhibits increased therapeutic activity in a model of disseminated tuberculosis. Int J Antimicrob Agents, 2008. 31(1): p. 37-45.
| Antibacterial experiment [1]: | |
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Bacteria |
M. abscessus subspecies |
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Preparation method |
The solubility of this compound in DMSO is > 42.4 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0.1 or 0.5 μM (MIC90s) |
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Applications |
Pretreating M. abscessus subspecies abscessus and bolletii with 0.5 μM Rifabutin, as well as M. abscessus subspecies massiliense with 0.1 μM Rifabutin did not affect the MIC90s, which implied that M. abscessus did not have inducible Rifabutin resistance mechanisms. In addition, at the doses which are 2-fold of the MIC90s, Rifabutin showed similar or higher bactericidal activities than Clarithromycin. |
| Animal experiment [2]: | |
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Animal models |
Mice inoculated with tachyzoites or cysts of Toxoplasma gondii |
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Dosage form |
50, 100, 200, 300 or 400 mg/kg; p.o.; q.d., for 10 days |
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Applications |
In mice inoculated with tachyzoites or cysts of Toxoplasma gondii, 300 mg/kg and 400 mg/kg Rifabutin protected all infected mice against death. At the doses of 100 mg/kg and 200 mg/kg, Rifabutin protected 80% and 10 ~ 40% of the infected mice against death, respectively. However, at the dose of 50 mg/kg, Rifabutin only induced a delay in time to death. |
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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]. Aziz DB, Low JL, Wu ML, Gengenbacher M, Teo JWP, Dartois V, Dick T. Rifabutin Is Active against Mycobacterium abscessus Complex. Antimicrob Agents Chemother. 2017 May 24;61(6). [2]. Araujo FG, Slifer T, Remington JS. Rifabutin is active in murine models of toxoplasmosis. Antimicrob Agents Chemother. 1994 Mar;38(3):570-5. |
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| Cas No. | 72559-06-9 | SDF | |
| 别名 | 利福布丁; Ansamycin; LM-427 | ||
| Canonical SMILES | O[C@H]([C@H](C)[C@@H](O)[C@@H](C)/C=C/C=C(C)\C(NC1=C2C3=NC4(CCN(CC(C)C)CC4)N2)=O)[C@@H](C)[C@H](OC(C)=O)[C@H](C)[C@@H](OC)/C=C/O[C@@]5(C)OC6=C(C5=O)C3=C(C(O)=C6C)C1=O | ||
| 分子式 | C46H62N4O11 | 分子量 | 847 |
| 溶解度 | ≥ 42.35mg/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 | 1.1806 mL | 5.9032 mL | 11.8064 mL |
| 5 mM | 0.2361 mL | 1.1806 mL | 2.3613 mL |
| 10 mM | 0.1181 mL | 0.5903 mL | 1.1806 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet