Rifabutin (LM427)

Synonyms: LM427, Ansamycin

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

Rifabutin (LM427) Chemical Structure

Rifabutin (LM427) Chemical Structure

CAS No. 72559-06-9

Purity & Quality Control

Rifabutin (LM427) Related Products

Biological Activity

Description Rifabutin (LM427, Ansamycin) is a semisynthetic ansamycin antibiotic, used in the treatment of Mycobacterium avium intracellulare (MAI) and tuberculosis.
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05684705 Recruiting
Bacterial Infections
BioVersys AG|CW-Research and Management GmbH
September 1 2023 Phase 1
NCT05684718 Completed
Bacterial Infections
BioVersys AG|CRU Hungary Kft
February 1 2023 Phase 1
NCT05537142 Recruiting
Healthy Participants
BioVersys AG|CRU Hungary Kft
September 2 2022 Phase 1
NCT04672525 Recruiting
Prosthetic Infection
Tourcoing Hospital
November 8 2021 Phase 3
NCT05086107 Completed
Renal Impairment
BioVersys AG|CRU Hungary Kft|CRU Hungary Early Phase Unit
October 8 2021 Phase 1

Chemical Information & Solubility

Molecular Weight 847 Formula

C46H62N4O11

CAS No. 72559-06-9 SDF Download Rifabutin (LM427) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (118.06 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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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 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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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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