Rifaximin

Catalog No.S1790

Rifaximin  Chemical Structure

Molecular Weight(MW): 785.88

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.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
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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

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

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]

Protocol

Solubility (25°C)

In vitro DMSO 47 mg/mL (59.8 mM)
Ethanol 3 mg/mL (3.81 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 785.88
Formula

C43H51N3O11

CAS No. 80621-81-4
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03529825 Recruiting Drug: Rifaximin Microbial Colonization Emory University July 18 2018 Early Phase 1
NCT04077125 Completed Drug: Rifaximin Minimal Hepatic Encephalopathy Fondazione Policlinico Universitario Agostino Gemelli IRCCS January 18 2018 --
NCT02555293 Recruiting Drug: XIFAXAN® (Rifaximin) Malignant Liver Disease|Major Liver Resection RWTH Aachen University February 2016 Phase 2

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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.

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DNA/RNA Synthesis Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID