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/ Rifabutin/利福布汀

Rifabutin/利福布汀 {[allProObj[0].p_purity_real_show]}

货号：A878035 同义名： 利福布丁 / Ansamycin; LM-427

Rifabutin是一种半合成的安莎霉素类抗生素，抑制 DNA 依赖性 RNA 聚合酶，主要用于结核病的治疗及预防鸟分枝杆菌感染。

Rifabutin/利福布汀 化学结构 CAS号：72559-06-9
Rifabutin/利福布汀 化学结构
CAS号：72559-06-9
Rifabutin/利福布汀 3D分子结构
CAS号：72559-06-9
Rifabutin/利福布汀 化学结构 CAS号：72559-06-9
Rifabutin/利福布汀 3D分子结构 CAS号：72559-06-9
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Rifabutin/利福布汀 纯度/质量文件 产品仅供科研

货号：A878035 标准纯度： {[allProObj[0].p_purity_real_show]}
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Rifabutin/利福布汀 生物活性

描述 Rifabutin (RBT) is the rifamycin that is recommended to treat tuberculosis (TB) in HIV-infected individuals during combination antiretroviral therapy (ART) containing HIV protease inhibitors (PIs)[3]. Rifabutin is a rifamycin with activity against Mycobacterium tuberculosis. RFB is well tolerated by patients who develop RMP-related (Rifampin) AEs (adverse effects)[4]. Rifabutin at 16 μg/mL was only bacteriostatic (MIC of 4 μg/mL) and was moderately synergistic in combination with imipenem (fractional inhibitory concentration [FIC] index of 0.38). Addition of rifabutin (16 μg/mL) moderately increased killing by a low (8 μg/mL) but not by a high (32 μg/mL) concentration of imipenem. In infected macrophages, rifabutin (16 μg/mL) increased the activity of imipenem at 8 and 32 μg/mL, achieving 3- and 100-fold reductions in the numbers of intracellular bacteria, respectively[5]. The use of rifabutin can improve treatment outcomes in patients with rifabutin-sensitive MDR-TB[6]. In addition, the combination of rifabutin plus bedaquiline produces sustained intracellular mycobactericidal activity that is greater than the sum of their individual effects[7].

Rifabutin/利福布汀 细胞实验

Cell Line
Concentration Treated Time Description References
LS180 cells 2 µM and 10 µM 6 days To evaluate the induction and inhibition of P-gp by Rifabutin. Results showed that Rifabutin significantly induced P-gp after 6-day exposure and significantly inhibited P-gp upon acute re-exposure, indicating its ability to partly counteract P-gp induction. Arch Toxicol. 2024 Jan;98(1):223-231.
Mycobacterium tuberculosis (Mtb72) 0.8 µg/ml 21 to 42 days To generate rifabutin-resistant mutants and measure their mutation frequency. Ann Clin Microbiol Antimicrob. 2005 Jun 15;4:9.
MRC5 fibroblasts 0.5 to 20 mg/ml 72 h Rifabutin alone inhibited Toxoplasma growth at concentrations between 0.5 and 20 mg/ml, with an estimated 50% inhibitory concentration of 1.68 mg/ml. Antimicrob Agents Chemother. 1996 Sep;40(9):2015-20.

Rifabutin/利福布汀 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice Non-tuberculous mycobacterial infection model Oral 20 mg/kg Once daily for 28 days To evaluate the antibacterial activity of Rifabutin against four common non-tuberculous mycobacteria, the results showed that Rifabutin did not inhibit M. avium and M. abscessus. Front Cell Infect Microbiol. 2023 Mar 22;13:1115530
Mice NOD SCID mice Oral gavage 10 mg/kg Once daily for 10 consecutive days To evaluate the efficacy of rifabutin in a murine model of NTM infection, results showed that rifabutin is bactericidal against M. abscessus K21 Antimicrob Agents Chemother. 2020 Jan 27;64(2):e01943-19
Mice Models of acute toxoplasmosis and toxoplasmic encephalitis Oral gavage 50-400 mg/kg Once daily for 10 days To evaluate the efficacy of rifabutin alone or in combination with other drugs in treating acute toxoplasmosis and toxoplasmic encephalitis in mice. Results showed that doses of 400 or 300 mg/kg of rifabutin protected 100% of the mice from death, doses of 200 mg/kg protected at least 80% of the mice, doses of 100 mg/kg protected 10-40% of the mice, and doses of 50 mg/kg were not protective but delayed time to death. When combined with other drugs, rifabutin significantly enhanced their in vivo activities. Antimicrob Agents Chemother. 1994 Mar;38(3):570-5
Mice Tuberculosis model Oral 10 mg/kg Once daily for 1.5 months To evaluate the bactericidal and sterilizing activity of Rifabutin in combination with Bedaquiline, Pyrazinamide, and Moxifloxacin. Results showed that BZMRb significantly reduced the relapse rate in BALB/c mice after 1.5 months of treatment, and in the C3HeB/FeJ mouse model, BZMRb demonstrated superior sterilizing activity compared to PZMH after 2 months of treatment. Antimicrob Agents Chemother. 2022 Apr 19;66(4):e0239821
BALB/c mice Mouse model of tuberculosis preventive therapy (TPT) Oral 0.3, 1, 3 mg/kg Once daily, 5 days per week for 2 weeks To evaluate the pharmacokinetic and pharmacodynamic relationships of rifabutin under simulated long-acting injectable (LAI) exposures to guide the development of LAI formulations. Results showed significant bactericidal activity when rifabutin plasma concentrations were maintained above target levels. Antimicrob Agents Chemother. 2023 Jul 18;67(7):e0048123
Mice Acute toxoplasmosis model Oral 200 mg/kg Once daily for 10 days Rifabutin alone administered from day 1 to day 10 postinfection resulted in 100% protection during treatment, with clearance of parasites from the blood, brain, and lungs. After cessation of therapy, relapses occurred in the brain and lungs; mortality was 46% at the end of the experiment (day 30). Antimicrob Agents Chemother. 1996 Sep;40(9):2015-20.
Mice Tuberculosis model Oral 10 mg/kg Daily for 12 weeks To evaluate the efficacy of rifabutin alone or in combination with isoniazid in preventing tuberculosis in mice. Results showed that rifabutin was highly effective as early as the eighth week of treatment: all spleens were sterilized, and the number of bacteria was drastically reduced in the lungs. After 12 weeks of treatment, no bacilli were found in the spleens or lungs of any of the animals. Antimicrob Agents Chemother. 1994 Oct;38(10):2346-50

Rifabutin/利福布汀 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02024555 Sarcoidosis; Antimycobacterial... 展开 >> Therapy 收起 << Phase 2 Recruiting May 2019 United States, New York ... 展开 >> Albany Medical Center Recruiting Albany, New York, United States, 12208 Contact: Marc Judson, MD    518-262-5196    judsonm@mail.amc.edu    Contact: Leahruth Saavedra, MS    (518) 262-0355    saavedl@amc.edu    Sub-Investigator: Marc Judson, MD          United States, Ohio University of Cincinnati Recruiting Cincinnati, Ohio, United States, 45267 Contact: Robert Baughman, MD    513-584-5110    bob.baughman@ucmail.uc.edu    Contact: Joyce Zeigler    (513) 584-6252    zeiglejm@ucmail.uc.edu    Principal Investigator: Robert Baughman, MD          Cleveland Clinic Recruiting Cleveland, Ohio, United States, 44195 Contact: Dan Culver, DO    216-444-6508    culverd@ccf.org    Contact: Allison Wimer    216-444-9975    wimera@ccf.org    Principal Investigator: Dan Culver, DO          Ohio State University Recruiting Columbus, Ohio, United States, 43221 Contact: Elliott Crouser, M.D.    614-293-4925    elliott.crouser@osumc.edu    Contact: Karen Martin    614-293-4978    karen.martin@osumc.edu    Sub-Investigator: Elliott Crouser, M.D.          United States, South Carolina Medical University of South Carolina Recruiting Charleston, South Carolina, United States, 29425 Contact: Ennis James, MD    843-792-3769    jamesw@musc.edu    Contact: Robyn Do    (843) 792-1221    dorobyn@musc.edu    Sub-Investigator: Ennis James, MD          United States, Tennessee Vanderbilt University School of Medicine Recruiting Nashville, Tennessee, United States, 37232 Contact: Wonder Drake, MD    615-322-2035    wonder.drake@vanderbilt.edu    Contact: Amy Kerrigan, MSN    615-343-3238    amy.kerrigan@vanderbilt.edu    Principal Investigator: Wonder Drake, MD 收起 <<
NCT02099240 Osteomyelitis Early Phase 1 Recruiting September 2019 United States, Kentucky ... 展开 >> University of Louisville Recruiting Louisville, Kentucky, United States, 40202 Contact: Julio A Ramirez, MD    502-852-1148    jarami01@louisville.edu    Contact: David Seligson, MD    502-852-0923    d0seli01@louisville.edu    Sub-Investigator: Forest Arnold, DO          Sub-Investigator: Timothy Wiemkwn, PhD          Sub-Investigator: Robert Kelley, PhD          Sub-Investigator: James Summersgill, PhD          Sub-Investigator: Ruth Carrico, PhD          Sub-Investigator: Julie Harting, PharmD          Sub-Investigator: Paula Peyrani, MD          Principal Investigator: David Seligson, MD          Sub-Investigator: Craig Roberts, MD          Principal Investigator: Julio Ramirez, MD 收起 <<
NCT01951326 Crohn's Disease Phase 3 Active, not recruiting April 2019 -

Rifabutin/利福布汀 参考文献

[1]Katoh M, Watanabe M, et al. In vivo induction of human cytochrome P450 3A4 by rifabutin in chimeric mice with humanized liver. Xenobiotica. 2005 Sep;35(9):863-75.

[2]Kunin CM. Antimicrobial activity of rifabutin. Clin Infect Dis. 1996 Apr;22 Suppl 1:S3-13; discussion S13-4.

[3]Ramachandran G, Hemanth Kumar AK, Kannan T, et al. Pharmacokinetics of rifabutin during atazanavir/ritonavir co-administration in HIV-infected TB patients. Indian J Tuberc. 2019;66(1):129–133

[4]Horne DJ, Spitters C, Narita M. Experience with rifabutin replacing rifampin in the treatment of tuberculosis. Int J Tuberc Lung Dis. 2011;15(11):1485–i

[5]Le Run E, Arthur M, Mainardi JL. In Vitro and Intracellular Activity of Imipenem Combined with Rifabutin and Avibactam against Mycobacterium abscessus. Antimicrob Agents Chemother. 2018;62(8):e00623-18.

[6]Lee H, Ahn S, Hwang NY, et al. Treatment outcomes of rifabutin-containing regimens for rifabutin-sensitive multidrug-resistant pulmonary tuberculosis. Int J Infect Dis. 2017;65:135–141

[7]Wallis RS, Good CE, O'Riordan MA, et al. Mycobactericidal activity of bedaquiline plus rifabutin or rifampin in ex vivo whole blood cultures of healthy volunteers: A randomized controlled trial. PLoS One. 2018;13(5):e0196756. Published 2018 May 2

Rifabutin/利福布汀 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.18mL

0.24mL

0.12mL

5.90mL

1.18mL

0.59mL

11.81mL

2.36mL

1.18mL

Rifabutin/利福布汀 技术信息

CAS号72559-06-9
分子式C46H62N4O11
分子量 847.0
SMILES Code C[C@@]1(O2)O/C=C/[C@@H]([C@H]([C@H]([C@H](C)[C@H](O)[C@H](C)[C@H]([C@H](/C=C/C=C(C(NC(C3=O)=C4NC5(CCN(CC(C)C)CC5)N=C4C6=C3C(O)=C(C)C2=C6C1=O)=O)\C)C)O)OC(C)=O)C)OC
MDL No. MFCD00866816
别名 利福布丁 ;Ansamycin; LM-427; Rifabutina; Mycobutin
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C
溶解方案

DMSO: 50 mg/mL(59.03 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一

Tags: Rifabutin | Ansamycin;LM-427;Rifabutina;Mycobutin | 利福布丁 | Ansamycin | Antibacterial | AmBeed-信号通路专用抑制剂 | Rifabutin/利福布汀 纯度/质量文件 | Rifabutin/利福布汀 生物活性 | Rifabutin/利福布汀 临床数据 | Rifabutin/利福布汀 参考文献 | Rifabutin/利福布汀 实验方案 | Rifabutin/利福布汀 技术信息

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