Rifamycin
Based on 2 publication(s) in Google Scholar
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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- Pureza: 98.06%
- No. CAS: 6998-60-3
- Fòrmula: C37H47NO12
- Peso molecular:697.77
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Rifamycin
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Cancer cell lines | GI50 |
10 μM
Compound: Rifamycin SV
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Growth inhibition of human Colon cancer cells
Growth inhibition of human Colon cancer cells
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[PMID: 25205189] |
| Cancer cell lines | GI50 |
10 μM
Compound: Rifamycin SV
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Growth inhibition of human Prostate cancer cells
Growth inhibition of human Prostate cancer cells
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[PMID: 25205189] |
| Cancer cell lines | GI50 |
15.9 μM
Compound: Rifamycin SV
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Growth inhibition of human Renal cancer cells
Growth inhibition of human Renal cancer cells
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[PMID: 25205189] |
| Cancer cell lines | GI50 |
16.6 μM
Compound: Rifamycin SV
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Growth inhibition of human Breast cancer cells
Growth inhibition of human Breast cancer cells
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[PMID: 25205189] |
| Cancer cell lines | GI50 |
18.6 μM
Compound: Rifamycin SV
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Growth inhibition of human Ovarian cancer cells
Growth inhibition of human Ovarian cancer cells
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[PMID: 25205189] |
| Cancer cell lines | GI50 |
21.4 μM
Compound: Rifamycin SV
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Growth inhibition of human CNS cancer cells
Growth inhibition of human CNS cancer cells
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[PMID: 25205189] |
| HEK293 | IC50 |
0.23 μM
Compound: Rifamycin SVd
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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
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[PMID: 15616150] |
| Leukemia cell | GI50 |
3.2 μM
Compound: Rifamycin SV
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Growth inhibition of human Leukemia cells
Growth inhibition of human Leukemia cells
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[PMID: 25205189] |
| Melanoma cell | GI50 |
15.5 μM
Compound: Rifamycin SV
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Growth inhibition of human Melanoma cells
Growth inhibition of human Melanoma cells
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[PMID: 25205189] |
| NSCLC | GI50 |
14.5 μM
Compound: Rifamycin SV
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Growth inhibition of human NSCLC cells
Growth inhibition of human NSCLC cells
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[PMID: 25205189] |
| Sf21 | IC50 |
3.1 μM
Compound: Rifamycin SV
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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
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[PMID: 21965623] |
| Sf21 | IC50 |
6.3 μM
Compound: Rifamycin SV
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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
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[PMID: 21965623] |
| Vero | CC50 |
62.46 μg/mL
Compound: RFM
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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
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[PMID: 23474387] |
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.
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.
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Animal Model:Male Wistar rats (weight 200-250 g), cecal ligation puncture (CLP)-induced intra-abdominal infection model[6]
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Dosage:25 mg/kg, 12.5 mg/kg
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Administration:Peritoneal lavage
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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).
Chemical Information
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No. CAS 6998-60-3
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Appearance Solid
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Peso molecular 697.77
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Fòrmula C37H47NO12
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Color Light yellow to brown
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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
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Synonyms
Rifamycin SV
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
2026 Mar;13(16):e13310. PMID: 41589654 -
Proc Natl Acad Sci U S A
Structure-guided approach to modulate small molecule binding to a promiscuous ligand-activated protein. [Abstract]2023 Mar 7;120(10):e2217804120. PMID: 36848571
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (289 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Floss HG, et al. Rifamycin-mode of action, resistance, and biosynthesis. Chem Rev. 2005 Feb;105(2):621-32. [Content Brief]
[2]. Fattinger K, et al. Rifamycin SV and rifampicin exhibit differential inhibition of the hepatic rat organic anion transporting polypeptides, Oatp1 and Oatp2. Hepatology. 2000 Jul;32(1):82-6. [Content Brief]
[3]. Rosette C, et al. Anti-inflammatory and immunomodulatory activities of rifamycin SV. Int J Antimicrob Agents. 2013 Aug;42(2):182-6. [Content Brief]
[5]. Saito K, et al. Rifamycin action on RNA polymerase in antibiotic-tolerant Mycobacterium tuberculosis results in differentially detectable populations. Proc Natl Acad Sci U S A. 2017 Jun 13;114(24):E4832-E4840. [Content Brief]
[6]. Jallouli M, et al. Rifamycin lavage in the treatment of experimental intra-abdominal infection. J Surg Res. 2009 Aug;155(2):191-4. [Content Brief]
[7]. Zhang M, et al. Treatment of tuberculosis with rifamycin-containing regimens in immune-deficient mice. Am J Respir Crit Care Med. 2011 May 1;183(9):1254-61. [Content Brief]
[8]. Omansen TF, et al. High-Dose Rifamycins Enable Shorter Oral Treatment in a Murine Model of Mycobacterium ulcerans Disease. Antimicrob Agents Chemother. 2019 Jan 29;63(2):e01478-18. [Content Brief]
[10]. Okolicsanyi L, et al. Influence of rifamycin SV on bile acid metabolism in rats. Naunyn Schmiedebergs Arch Pharmacol. 1980 Aug;313(2):171-4. [Content Brief]
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 |
Rifamycin Related Classifications
HY-B1907A Related Classifications
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