Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor Rifaximin For research use only.

Rifaximin

Rifaximin is a RNA synthesis inhibitor by binding the β subunit of the bacterial DNA-dependent RNA polymerase, used to treat traveler's diarrhea caused by certain bacteria.

Rifaximin Chemical Structure

Rifaximin Chemical Structure

CAS No. 80621-81-4

Purity & Quality Control

Rifaximin Related Products

Signaling Pathway

DNA/RNA Synthesis Signaling Pathways

DNA/RNA Synthesis Signaling Pathway

Biological Activity

Description Rifaximin is a RNA synthesis inhibitor by binding the β subunit of the bacterial DNA-dependent RNA polymerase, used to treat traveler's diarrhea caused by certain bacteria.
Targets
RNA polymerase [1]
In vitro
In vitro

Rifaximin (50 μM) reduces changes in the production of proinflammatory factors caused by LPS stimulation in IEC, such as TNF-α, IL-8, Rantes and PGE2 in normal intestinal epithelial cells. Rifaximin inhibits the LPS-induced cytokine and chemokine expression by suppressing NF-κB DNA-binding activity. Rifaximin (100 μM) effectively decreases the expression of TNFα, IL-8, MIP-3α and Rantes induced by LPS stimulation (100 μg/mL). [1] Rifaximin binds the β subunit of the bacterial DNA-dependent RNA polymerase, inhibiting the initiation of chain formation in RNA synthesis. Rifaximin has a lower MIC against gram-positive bacteria, with an MIC90 at dosages ranging from 0.01 µg/mL to 0.5 µg/mL. Rifaximin has broad-spectrum activity against aerobic and anaerobic gram-positive and gram-negative microorganisms. [2]
In Vivo
In vivo

Rifaximin is highly concentrated in the intestinal tract compared with rifampicin. Rifaximin treatment results in significant induction of PXR target genes in the intestine of hPXR mice, but not in wild-type and Pxr-null mice. Rifaximin-mediated activation of human PXR, but not the other xenobiotic nuclear receptors constitutive androstane receptor, peroxisome proliferator-activated receptor (PPAR)alpha, PPARgamma, and farnesoid X receptor. [3] Rifaximin could lead to PXR-dependent hepatocellular fatty degeneration as a result of activation of genes involved in lipid uptake, thus indicating a potential adverse effect of rifaximin on liver function after long-term exposure. [4]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05408910 Not yet recruiting
Cystic Fibrosis|Abdominal Pain|Small Bowel Disease
Wake Forest University Health Sciences|Nationwide Children''s Hospital|University of Minnesota|University of Texas Southwestern Medical Center
 July 2024 Phase 2|Phase 3
NCT06298409 Recruiting
Small Intestinal Bacterial Overgrowth
Envivo Bio Inc
 February 15 2024 --
NCT04244877 Withdrawn
Cirrhosis Liver|Minimal Hepatic Encephalopathy|Small Intestinal Bacterial Overgrowth|Gastrointestinal Motility Disorder
MetroHealth Medical Center
 September 15 2021 Phase 3

Chemical Information & Solubility

Molecular Weight 785.88 Formula

C43H51N3O11
CAS No. 80621-81-4 SDF Download Rifaximin SDF
Smiles CC1C=CC=C(C(=O)NC2=C(C3=C(C4=C(C(=C3O)C)OC(C4=O)(OC=CC(C(C(C(C(C(C1O)C)O)C)OC(=O)C)C)OC)C)C5=C2N6C=CC(=CC6=N5)C)O)C
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 157 mg/mL

DMSO : 47 mg/mL ( (59.8 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

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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