Rifabutin (Synonyms: Ansamycin, LM-427) |
Catalog No.GC15046
One-Click Copy Product Info
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anti-TB(tuberculosis) medicine
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Synonyms | 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 | ||
| Formula | C46H62N4O11 | M.Wt | 847 |
| Solubility | ≥ 42.35mg/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 | 1.1806 mL | 5.9032 mL | 11.8064 mL |
| 5 mM | 236.1 μL | 1.1806 mL | 2.3613 mL |
| 10 mM | 118.1 μL | 590.3 μL | 1.1806 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 saline, 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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)