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Rifaximin DNA/RNA Synthesis inhibitor

Name: Rifaximin
SKU: S1790
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S1790

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.

Chemical Structure

Molecular Weight: 785.88

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.98%

99.98

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Chemical Information, Storage & Stability

Molecular Weight	785.88	Formula	C₄₃H₅₁N₃O₁₁	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	80621-81-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Solubility

In vitro
Batch:

Ethanol : 157 mg/mL

DMSO : 47 mg/mL (59.8 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.

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.

Mechanism of Action

Targets/IC₅₀/Ki	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. This compound inhibits the LPS-induced cytokine and chemokine expression by suppressing NF-κB DNA-binding activity. It (100 μM) effectively decreases the expression of TNFα, IL-8, MIP-3α and Rantes induced by LPS stimulation (100 μg/mL). ^[1] This chemical binds the β subunit of the bacterial DNA-dependent RNA polymerase, inhibiting the initiation of chain formation in RNA synthesis. It has a lower MIC against gram-positive bacteria, with an MIC90 at dosages ranging from 0.01 µg/mL to 0.5 µg/mL. This agent 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. This compound treatment results in significant induction of PXR target genes in the intestine of hPXR mice, but not in wild-type and Pxr-null mice. This chemical-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] It 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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/21806984/ [2] https://pubmed.ncbi.nlm.nih.gov/16421799/ [3] https://pubmed.ncbi.nlm.nih.gov/17442842/ [4] https://pubmed.ncbi.nlm.nih.gov/22790967/

Clinical Trial Information

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

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

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