1. Anti-infection Cell Cycle/DNA Damage
  2. Antibiotic Bacterial DNA/RNA Synthesis
  3. Rifamycin

Rifamycin (Rifamycin SV) is an orally active ansamycin antibiotic. Rifamycin inhibits DNA-dependent RNA synthesis. Rifamycin has antibacterial activity against Mycobacterium tuberculosis. Rifamycin interferes with hepatic bile acid metabolism. Rifamycin has anti-inflammatory effects. Rifamycin can be used in the study of Mycobacterium tuberculosis, Bacteroides fragilis infection, and Lipopolysaccharide (HY-D1056B3)-induced inflammation.

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Rifamycin

Rifamycin Chemical Structure

CAS No. : 6998-60-3

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10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 2 publication(s) in Google Scholar

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Description

Rifamycin (Rifamycin SV) is an orally active ansamycin antibiotic. Rifamycin inhibits DNA-dependent RNA synthesis. Rifamycin has antibacterial activity against Mycobacterium tuberculosis. Rifamycin interferes with hepatic bile acid metabolism. Rifamycin has anti-inflammatory effects. Rifamycin can be used in the study of Mycobacterium tuberculosis, Bacteroides fragilis infection, and Lipopolysaccharide (HY-D1056B3)-induced inflammation[1][2][3][4][5][6][7][8][9][10][11].

Cellular Effect
Cell Line Type Value Description References
Cancer cell lines GI50
10 μM
Compound: Rifamycin SV
Growth inhibition of human Colon cancer cells
Growth inhibition of human Colon cancer cells
[PMID: 25205189]
Cancer cell lines GI50
10 μM
Compound: Rifamycin SV
Growth inhibition of human Prostate cancer cells
Growth inhibition of human Prostate cancer cells
[PMID: 25205189]
Cancer cell lines GI50
15.9 μM
Compound: Rifamycin SV
Growth inhibition of human Renal cancer cells
Growth inhibition of human Renal cancer cells
[PMID: 25205189]
Cancer cell lines GI50
16.6 μM
Compound: Rifamycin SV
Growth inhibition of human Breast cancer cells
Growth inhibition of human Breast cancer cells
[PMID: 25205189]
Cancer cell lines GI50
18.6 μM
Compound: Rifamycin SV
Growth inhibition of human Ovarian cancer cells
Growth inhibition of human Ovarian cancer cells
[PMID: 25205189]
Cancer cell lines GI50
21.4 μM
Compound: Rifamycin SV
Growth inhibition of human CNS cancer cells
Growth inhibition of human CNS cancer cells
[PMID: 25205189]
HEK293 IC50
0.23 μM
Compound: Rifamycin SVd
TP_TRANSPORTER: inhibition of estradiol-17beta-glucuronide uptake(estradiol-17beta-glucuronide:0.02uM) in OATP1B1-expressing HEK293 cells
TP_TRANSPORTER: inhibition of estradiol-17beta-glucuronide uptake(estradiol-17beta-glucuronide:0.02uM) in OATP1B1-expressing HEK293 cells
[PMID: 15616150]
Leukemia cell GI50
3.2 μM
Compound: Rifamycin SV
Growth inhibition of human Leukemia cells
Growth inhibition of human Leukemia cells
[PMID: 25205189]
Melanoma cell GI50
15.5 μM
Compound: Rifamycin SV
Growth inhibition of human Melanoma cells
Growth inhibition of human Melanoma cells
[PMID: 25205189]
NSCLC GI50
14.5 μM
Compound: Rifamycin SV
Growth inhibition of human NSCLC cells
Growth inhibition of human NSCLC cells
[PMID: 25205189]
Sf21 IC50
3.1 μM
Compound: Rifamycin SV
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
[PMID: 21965623]
Sf21 IC50
6.3 μM
Compound: Rifamycin SV
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
[PMID: 21965623]
Vero CC50
62.46 μg/mL
Compound: RFM
Cytotoxicity against african green monkey Vero cells after 72 hrs by resazurin assay
Cytotoxicity against african green monkey Vero cells after 72 hrs by resazurin assay
[PMID: 23474387]
In Vitro

Rifamycin (10 μM; 30 s) mainly inhibits -independent Taurocholate (HY-N0545) uptake in short-term cultured rat hepatocytes[2].
Rifamycin (10-100 μM; 15 min) effectively inhibits Oatp2-mediated Taurocholate uptake in Xenopus oocytes expressing Na+/Ntcp[2].
Rifamycin (1-100 μM; 24 h) inhibits the synthesis of cytokines and chemokines from lipopolysaccharide-activated monocytes and macrophages[3].
Rifamycin (0.16 μg/ml; 2 weeks of culture) inhibits the growth of M. tuberculosis and its drug-resistant mutants in TB broth containing 10% serum albumin[4].

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

In Vivo

Rifamycin (5 mg/day; s.c.; 3 days a week) is effective in mice infected with M. tuberculosis, significantly reducing the number of viable bacteria in the body[4].
Rifamycin (12.5-25 mg/kg; peritoneal lavage) can improve the survival rate of rats with experimental intraperitoneal infection and significantly reduce the number of intraperitoneal bacteria and adhesion formation[6].
Rifamycin (5-40 mg/kg; esophageal gavage; once a day, 5 days a week; 4 weeks) shortens oral treatment duration in a mouse model of Mycobacterium ulcerans disease[8].
Rifamycin (0.1 mL; intraaural administration; twice daily; 10 days) does not cause hearing loss in adult or weanling rats[9].
Rifamycin (1 mg i.v. bolus followed by 4 mg i.v. infusion; 70 min) interferes with three major steps of Bile acid metabolism in rats with intravenous Sodium cholate (HY-N0324A) infusion, resulting in a significant decrease in bile acid uptake and excretion[10].
Rifamycin (10-160 mg/kg; s.c.; single dose) is approximately 11 times less effective than Metronidazole (HY-B0318) in a mouse Bacteroides fragilis thigh infection model[11].

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

Animal Model: Male Wistar rats (weight 200-250 g), cecal ligation puncture (CLP)-induced intra-abdominal infection model[6]
Dosage: 25 mg/kg, 12.5 mg/kg
Administration: Peritoneal lavage
Result: Improved survival from 50% in the control group to 91.7% in the 25 mg/kg group and 100% in the 12.5 mg/kg group.
Significantly reduced adhesion formation.
Showed a greater reduction in bacterial counts in peritoneal fluid (25 mg/kg).
Molecular Weight

697.77

Formula

C37H47NO12

CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

C[C@H]1/C=C/C=C(C)\C(NC2=CC(O)=C3C(C(O)=C(C)C4=C3C([C@](O/C=C/[C@H](OC)[C@@H](C)[C@@H](OC(C)=O)[C@H](C)[C@H](O)[C@H](C)[C@H]1O)(C)O4)=O)=C2O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (143.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4331 mL 7.1657 mL 14.3314 mL
5 mM 0.2866 mL 1.4331 mL 2.8663 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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: ≥ 5 mg/mL (7.17 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (7.17 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Purity & Documentation
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4331 mL 7.1657 mL 14.3314 mL 35.8284 mL
5 mM 0.2866 mL 1.4331 mL 2.8663 mL 7.1657 mL
10 mM 0.1433 mL 0.7166 mL 1.4331 mL 3.5828 mL
15 mM 0.0955 mL 0.4777 mL 0.9554 mL 2.3886 mL
20 mM 0.0717 mL 0.3583 mL 0.7166 mL 1.7914 mL
25 mM 0.0573 mL 0.2866 mL 0.5733 mL 1.4331 mL
30 mM 0.0478 mL 0.2389 mL 0.4777 mL 1.1943 mL
40 mM 0.0358 mL 0.1791 mL 0.3583 mL 0.8957 mL
50 mM 0.0287 mL 0.1433 mL 0.2866 mL 0.7166 mL
60 mM 0.0239 mL 0.1194 mL 0.2389 mL 0.5971 mL
80 mM 0.0179 mL 0.0896 mL 0.1791 mL 0.4479 mL
100 mM 0.0143 mL 0.0717 mL 0.1433 mL 0.3583 mL
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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.

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Rifamycin
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