2. Anti-infection Cell Cycle/DNA Damage
  3. Bacterial Antibiotic DNA/RNA Synthesis
  4. Rifaximin

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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Rifaximin

Rifaximin 화학구조

CAS No. : 80621-81-4

사이즈 가격 재고 수량
무료 샘플 (0.1 - 0.2 mg)   지금 신청하기  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
500 mg 해외재고보유
1 g 해외재고보유
5 g 해외재고보유
10 g   견적 받기  
50 g   견적 받기  

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 8 publication(s) in Google Scholar

Other Forms of Rifaximin:

Rifaximin Related Antibodies

Top Publications Citing Use of Products

View All Antibiotic Isoform Specific Products:

View All Isoforms
Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

View All DNA/RNA Synthesis Isoform Specific Products:

View All Isoforms
RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

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)[1][2].

IC50 & Target

RNA Polymerase

 

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.

Rifaximin Related Antibodies

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
분자량

785.88

화학식

C43H51N3O11
CAS No.
Appearance

Solid

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
선적

Room temperature in continental US; may vary elsewhere.
보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
용액&용해도
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2725 mL 6.3623 mL 12.7246 mL
5 mM 0.2545 mL 1.2725 mL 2.5449 mL
View the Complete Stock Solution Preparation Table

* 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.

  • 몰농도 계산기

  • 농도 희석 계산기

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서

Purity: 99.64%

SDS (394 KB)

COA (256 KB) HNMR (301 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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
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Rifaximin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rifaximin80621-81-4BacterialAntibioticDNA/RNA SynthesisantibioticgastrointestinalbacterialinfectiondiarrheaInhibitorinhibitorinhibit

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상품명:
Rifaximin
Cat. No.:
HY-13234
수량:
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SAFETY DATA SHEET (SDS)

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