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Rifabutin

现货
Catalog No.
B2126
抗结核药物
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 600.00
现货
50mg
¥ 680.00
现货
100mg
¥ 1,000.00
现货
500mg
¥ 2,470.00
现货

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Background

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt847
Cas No.72559-06-9
FormulaC46H62N4O11
Solubility≥42.35mg/mL in DMSO
SDFDownload SDF
Canonical SMILESO[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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

抗菌实验 [1]:

细菌系

脓肿分枝杆菌亚种

制备方法

在DMSO中的溶解度大于42.4 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

0.1或0.5 μM (MIC90s)

实验结果

使用0.5 μM Rifabutin预处理脓肿分枝杆菌亚种abscessus和bolletii,使用0.1 μM Rifabutin预处理脓肿分枝杆菌亚种massiliense。上述预处理不影响MIC90s。因此,脓肿分枝杆菌可能不具有可诱导的Rifabutin抗性机制。此外,在2倍MIC90s的剂量下,与Clarithromycin相比,Rifabutin显示出相似或更高的杀菌活性。

动物实验 [2]:

动物模型

接种了弓形虫速殖子或囊肿的小鼠

给药剂量

50、100、200、300或400 mg/kg;口服给药;每天1次,持续10天

实验结果

在接种了弓形虫速殖子或囊肿的小鼠中,300 mg/kg和400 mg/kg Rifabutin使所有感染小鼠免于死亡。在100 mg/kg和200 mg/kg的剂量下,Rifabutin分别保护80%和10 ~ 40%的感染小鼠免于死亡。然而,在剂量为50 mg/kg时,Rifabutin仅能引起死亡时间延迟。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

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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