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

Jump to

Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	Integrase Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite Reverse Transcriptase HIV
Other Antineoplastic and Immunosuppressive Antibiotics Inhibitors	Staurosporine (STS) Cyclosporin A Oligomycin A (MCH 32) Puromycin Dihydrochloride Nigericin sodium salt Geldanamycin (NSC 122750) Honokiol Streptozotocin (STZ) Sodium Monensin (NSC 343257) Cephalomannine

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (118.06 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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

+

%

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 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.

Chemical Information, Storage & Stability

Molecular Weight	847	Formula	C₄₆H₆₂N₄O₁₁	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	72559-06-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LM427, Ansamycin			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

Mechanism of Action

In vitro	Rifabutin (LM427) has a broad spectrum of antimicrobial activity and is considerably more active than rifampin in vitro against the Mycobacterium avium complex (MAC), Mycobacterium tuberculosis, and Mycobacterium leprae. It also is active against most atypical mycobacteria, including Mycobacterium kansasii, but Mycobacterium chelonae is relatively resistant. This compound 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. It 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. It enhances the glucuronidation of 1-naphthol, 4-hydroxybiphenyl and beta-estradiol by a factor of two to three.
In vivo	Rifabutin (LM427) 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. When combined with Pyrimethamine (10 mg/kg), this compound (100 mg/kg) protects 75% of the mice infected with a lethal inoculum of tachyzoites or cysts of Toxoplasma gondii against death.
References	[1] https://pubmed.ncbi.nlm.nih.gov/8785253/ [2] https://pubmed.ncbi.nlm.nih.gov/8836814/ [3] https://pubmed.ncbi.nlm.nih.gov/16308281/ [4] https://pubmed.ncbi.nlm.nih.gov/8203856/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Rifabutin (LM427) Antineoplastic and Immunosuppressive Antibiotics inhibitor

Chemical Structure

Molecular Weight: 847