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Rifabutin (LM427)

Name: Rifabutin (LM427)
Brand: Selleck Chemicals
SKU: S1741
Rating: 5 (8 reviews)

Synonyms: LM427, Ansamycin

Catalog No.S1741 Purity: 99.99%

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

Rifabutin (LM427) Chemical Structure

CAS: 72559-06-9

Selleck's Rifabutin (LM427) has been cited by 8 publications

Purity & Quality Control

Batch: Purity: 99.99%

99.99

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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
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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

[4] Araujo FG, et al. Antimicrob Agents Chemother, 1994, 38(3), 570-575.

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Chemical lnformation & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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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 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.
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.

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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