Art. -Nr.: HY-13234

Rifaximin

8 Cited Publications

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Based on 8 publication(s) in Google Scholar

Rifaximin, a gastrointestinal-selective antibiotic, binds the β-subunit of bacterial DNA-dependent RNA polymerase, resulting in inhibition of bacterial RNA synthesis. Rifaximin susceptibility is higher against Gram-positive strains (MIC: 0.03-5 mg/ml) compared to Gram-negative bacteria (MIC: 8-50 mg/mL).

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Reinheit: 99.64%
CAS. Nr.: 80621-81-4
Formel: C₄₃H₅₁N₃O₁₁
Molecular Weight:785.88

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Rifaximin Chemical Structure

CAS. Nr.: 80621-81-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

RNA Polymerase

Alle Antibiotic Isoform-spezifische Produkte anzeigen :

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	EC₅₀	11.2 μM Compound: Rifaximin	Transactivation of full length human PXR transfected in human HepG2 cells after 18 hrs by luciferase reporter assay relative to rifaximin Transactivation of full length human PXR transfected in human HepG2 cells after 18 hrs by luciferase reporter assay relative to rifaximin	[PMID: 26408814]
HepG2	EC₅₀	14.1 μM Compound: Rifaximin	Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis	[PMID: 20966043]
HepG2	EC₅₀	14.1 μM Compound: Rifaximin	Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis	[PMID: 20966043]
HepG2	EC₅₀	2.2 μM Compound: rifaximin	Transactivation of human PXR expressed in HepG2 cells after 18 hrs by luciferase reporter gene assay Transactivation of human PXR expressed in HepG2 cells after 18 hrs by luciferase reporter gene assay	[PMID: 21599020]
HepG2	EC₅₀	4 μM Compound: rifaximin	Agonist activity at human full-length PXR transfected in human HepG2 cells co-transfected with pSG5-RXR assessed as induction of transactivation by dual-luciferase reporter gene assay Agonist activity at human full-length PXR transfected in human HepG2 cells co-transfected with pSG5-RXR assessed as induction of transactivation by dual-luciferase reporter gene assay	[PMID: 24388834]

In Vitro

Rifaximin has a good inhibitory activity against Staphylococcus, Streptococcus, Enterococcus, Escherichia coli, Shigella, Salmonella, Bacillus cereus, Moraxella catarrhalis, Haemophilus influenzae, Haemophilus ducreyi, Bacteroides bivius-disiens, Gardnerella vaginalis, Lactobacillus spp.,Mobiluncus spp.,Neisseria gonorrhoeae, Pseudomonas and Acinetobacter . Rifaximin rarely causes side effects^[1].
Rifaximin (0.1, 1.0 and 10.0 μM) causes significant and concentration-dependent reduction of cell proliferation, cell migration and PCNA expression in the Caco-2 cells vs. untreated cells^[2].
Rifaximin (0.1-10 μM) downregulates Akt/mTOR and p38MAPK/NF-κB pathways through a PXR-dependent mechanism^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[2]

Cell Line:

Caco-2 cells
Concentration:

0.1, 1.0 and 10.0 μM
Incubation Time:

48 hours
Result:

Caused a significant and concentration-dependent reduction in cell proliferation. Reduced the expression of PCNA in a concentration-dependent manner.

Western Blot Analysis^[2]

Cell Line:

Caco-2 cells
Concentration:

0.1, 1.0 and 10.0 μM
Incubation Time:

24 hours
Result:

Reduced Akt, mTOR, p38 MAPK and HIF-1α expression in a concentration-dependent manner. Inhibited NF-κB nuclear activation and p70S6K.

In Vivo

Rifaximin administration (30 or 50 mg/kg/day) increases survival rates of colitic mice and reduces colitis severity by improvement of wasting syndrome, histologic scores, decrease in colon IL-2, IL-12, IFN-gamma and TNF-alpha (protein and mRNA) levels, and diminishes colon myeloperoxidase (MPO) activity^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Balb/c mice (6–8 weeks old) bearing 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis^[3]
Dosage:

10, 30 and 50 mg/kg/day
Administration:

Orally, p.o. daily for 7 days
Result:

Significantly reduced TNBS induced colitis at the dose of 30 and 50 mg/kg, but not 10 mg/kg. A 7-day course of 30 and 50 mg/kg resulted in an almost complete tissue protection.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 80621-81-4
Appearance Solid
Molecular Weight 785.88
Formel C₄₃H₅₁N₃O₁₁
Color Yellow to orange
SMILES

O=C1C2=C(O[C@@]1(O/C=C/[C@@H]([C@H]([C@H]([C@@H]([C@@H]([C@@H]([C@@H](O)[C@@H](C)/C=C/C=C(C)\C3=O)C)O)C)OC(C)=O)C)OC)C)C(C)=C(O)C4=C2C5=C(C(N3)=C4O)N6C(C=C(C)C=C6)=N5
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (8)

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Journal Impact Factor

J Exp Med

Antibiotic use in early life impairs MAIT cell-mediated immunity in adulthood. [Abstract]

2026 Mar 2;223(3):e20241287. PMID: 41400657
Phytomedicine

Sarsasapogenin stimulates angiogenesis and osteogenesis coupling to treat estrogen deficiency-induced osteoporosis by activating the GPX4/SLIT3/ROBO1 axis. [Abstract]

2024 Nov 28:136:156297. PMID: 39637471
Sci Rep

Mechanisms of rifaximin inhibition of hepatic fibrosis in mice with metabolic dysfunction associated steatohepatitis through the TLR4/NFκB pathway. [Abstract]

2025 Mar 21;15(1):9815. PMID: 40118973
Mol Pharm

Machine Learning Models Identify New Inhibitors for Human OATP1B1. [Abstract]

2022 Nov 7;19(11):4320-4332. PMID: 36269563
J Med Virol

Drug Repurposing: In Vitro Evaluation of Simeprevir as a Novel Antiviral Drug Against Severe Fever With Thrombocytopenia Syndrome Virus. [Abstract]

2025 Oct;97(10):e70655. PMID: 41117261
Brain Behav

The effect of rifaximin and lactulose treatments to chronic hepatic encephalopathy rats: An [18F]PBR146 in-vivo neuroinflammation imaging study. [Abstract]

2024 Jul;14(7):e3621. PMID: 38970239
Hong Kong Polytechnic University

2025.
bioRxiv

2024 May 10.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 50 mg/mL (63.62 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.2725 mL

6.3623 mL

12.7246 mL

5 mM

0.2545 mL

1.2725 mL

2.5449 mL

10 mM

0.1272 mL

0.6362 mL

1.2725 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 3 mg/mL (3.82 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 3 mg/mL (3.82 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (2.65 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Veronica Ojetti, et al. Rifaximin pharmacology and clinical implications. Expert Opin Drug Metab Toxicol. 2009 Jun;5(6):675-82. [Content Brief]

[2]. Giuseppe Esposito,et al. Rifaximin, a non-absorbable antibiotic, inhibits the release of pro-angiogenic mediators in colon cancer cells through a pregnane X receptor-dependent pathway. Int J Oncol. 2016 Aug;49(2):639-45. [Content Brief]

[3]. Stefano Fiorucci,et al.Inhibition of intestinal bacterial translocation with rifaximin modulates lamina propria monocytic cells reactivity and protects against inflammation in a rodent model of colitis. Digestion. 2002;66(4):246-56. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.2725 mL	6.3623 mL	12.7246 mL	31.8115 mL
	5 mM	0.2545 mL	1.2725 mL	2.5449 mL	6.3623 mL
	10 mM	0.1272 mL	0.6362 mL	1.2725 mL	3.1811 mL
	15 mM	0.0848 mL	0.4242 mL	0.8483 mL	2.1208 mL
	20 mM	0.0636 mL	0.3181 mL	0.6362 mL	1.5906 mL
	25 mM	0.0509 mL	0.2545 mL	0.5090 mL	1.2725 mL
	30 mM	0.0424 mL	0.2121 mL	0.4242 mL	1.0604 mL
	40 mM	0.0318 mL	0.1591 mL	0.3181 mL	0.7953 mL
	50 mM	0.0254 mL	0.1272 mL	0.2545 mL	0.6362 mL
	60 mM	0.0212 mL	0.1060 mL	0.2121 mL	0.5302 mL

Keywords

Rifaximin

8 Cited Publications

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Rifaximin

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Publications Citing Use of MedChemExpress (MCE) Rifaximin

Alle Antibiotic Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Rifaximin Related Classifications

HY-13234 Related Classifications