Rifabutin (LM427)

Catalog No.S1741 Synonyms: Ansamycin

For research use only.

Rifabutin (LM427, Ansamycin) is a semisynthetic ansamycin antibiotic, used in the treatment of Mycobacterium avium intracellulare (MAI) and tuberculosis.

Rifabutin (LM427) Chemical Structure

CAS No. 72559-06-9

Selleck's Rifabutin (LM427) has been cited by 5 Publications

Purity & Quality Control

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Biological Activity

Description Rifabutin (LM427, Ansamycin) is a semisynthetic ansamycin antibiotic, used in the treatment of Mycobacterium avium intracellulare (MAI) and tuberculosis.
In vitro

Rifabutin has a broad spectrum of antimicrobial activity. Rifabutin is considerably more active than rifampin in vitro against the Mycobacterium avium complex (MAC), Mycobacterium tuberculosis, and Mycobacterium leprae. Rifabutin also is active against most atypical mycobacteria, including Mycobacterium kansasii, but Mycobacterium chelonae is relatively resistant. Rifabutin also is active against staphylococci, group A streptococci, Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae, Haemophilus ducreyi, Campylobacter jejuni, Helicobacter pylori, Chlamydia trachomatis, and Toxoplasma gondii. [1] Rifabutin shows an isoenzyme-selectivity profile similar to that produced by Rifampicin, but the maximally achievable induction of cytochrome P-450 3A by Rifabutin is about two-fold lower compared with Rifampicin. Rifabutin enhances the glucuronidation of 1-naphthol, 4-hydroxybiphenyl and beta-estradiol by a factor of two to three. [2]

In vivo Rifabutin increases the human CYP3A4 mRNA expression, CYP3A4 protein content, testosterone 6ss-hydroxylase activity and dexamethasone 6-hydroxylase activity by 7.4-, 3.0-, 2.4- and 1.9-fold, respectively, in the chimeric mice. [3] Rifabutin (100 mg/kg) combined with Pyrimethamine (10 mg/kg) protects 75% of the mice infected with a lethal inoculum of tachyzoites or cysts of Toxoplasma gondii against death. [4]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 847


CAS No. 72559-06-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1C=CC=C(C(=O)N=C2C(=C3C(=C4C2=NC5(N4)CCN(CC5)CC(C)C)C6=C(C(=C3O)C)OC(C6=O)(OC=CC(C(C(C(C(C(C1O)C)O)C)OC(=O)C)C)OC)C)O)C

In vivo Formulation Calculator (Clear solution)

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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 ddH2O, 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.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04672525 Recruiting Drug: Rifabutin|Drug: Rifampicin Prosthetic Infection Tourcoing Hospital November 8 2021 Phase 3
NCT05086107 Recruiting Drug: BV100 Renal Impairment BioVersys AG|CRU Hungary Kft|CRU Hungary Early Phase Unit October 8 2021 Phase 1
NCT05087069 Active not recruiting Drug: BV100|Drug: Placebo Healthy Volunteers BioVersys SAS|Nuvisan GmbH|BioVersys AG October 8 2021 Phase 1
NCT04636983 Completed Drug: BV100|Drug: Placebo Healthy Subjects BioVersys SAS|BioVersys AG November 9 2020 Phase 1
NCT03891901 Recruiting Drug: Imatinib|Drug: Isoniazid|Drug: Rifabutin Tuberculosis National Institute of Allergy and Infectious Diseases (NIAID) October 27 2020 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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