| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| 5g |
|
||
| 10g | |||
| Other Sizes |
| Targets |
Rifamycin·Na targets bacterial DNA-dependent RNA polymerase, inhibiting DNA-dependent RNA synthesis. By binding to the β-subunit of RNA polymerase, it prevents the initiation of transcription, leading to bacterial cell death. It has antibacterial activity against Mycobacterium tuberculosis and other Gram-positive bacteria. Its mechanism of action is similar to that of rifampicin, another ansamycin antibiotic. The compound's effects on hepatic bile acid metabolism suggest interactions with liver function.
|
|---|---|
| ln Vitro |
In vitro, Rifamycin·Na has demonstrated antibacterial activity against Mycobacterium tuberculosis and Gram-positive bacteria. It inhibits DNA-dependent RNA synthesis. Its antibacterial activity is typically assessed using broth microdilution methods to determine minimum inhibitory concentrations (MIC). Its effects on bacterial RNA polymerase can be measured using in vitro transcription assays. These in vitro activities confirm its potential as an antibacterial agent and a tool for studying transcription.
|
| ln Vivo |
In vivo, Rifamycin·Na is effective in mice infected with M. tuberculosis at 5 mg/day administered subcutaneously 3 days a week. It is used to treat gastrointestinal infections due to its minimal oral absorption. After maternal use, rifamycin is unlikely to enter breast milk or the infant's bloodstream. Its effects on hepatic bile acid metabolism have been observed. These in vivo effects support its antibacterial activity and its potential for treating infections.
|
| Enzyme Assay |
For in vitro biochemical assays, Rifamycin·Na is evaluated for its antibacterial activity and RNA polymerase inhibition. Minimum inhibitory concentration (MIC) is determined using broth microdilution or agar dilution methods against bacterial strains including M. tuberculosis. RNA polymerase inhibition is measured using in vitro transcription assays with purified bacterial RNA polymerase and DNA templates. These cell-free and cell-based assays help characterize the compound's antibacterial activity and mechanism of action.
|
| Cell Assay |
In vitro cellular assays for Rifamycin·Na are performed using bacterial cultures. Bacteria including M. tuberculosis and Gram-positive strains are cultured in appropriate media and treated with the compound at various concentrations. Bacterial growth is monitored by measuring optical density or by colony counting. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) are determined. These cellular assays help validate the compound's antibacterial activity.
|
| Animal Protocol |
In vivo animal experiments with Rifamycin·Na are conducted in mouse models of tuberculosis infection. Mice infected with M. tuberculosis are treated with Rifamycin·Na at 5 mg/day administered subcutaneously 3 days a week. Efficacy endpoints include bacterial load reduction in lungs and survival. The compound's safety and tolerability are monitored through body weight, clinical signs, and histopathology. These studies help establish the compound's in vivo efficacy.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Rifamycin·Na have been characterized. The compound is minimally absorbed orally and is used only to treat gastrointestinal infections. After maternal use, it is unlikely to enter breast milk or the infant's bloodstream. The compound has a molecular weight of 719.75. It is soluble in water. Detailed PK parameters such as half-life, Cmax, Tmax, AUC, and protein binding are available in the pharmacological literature.
|
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation Rifampicin is minimally absorbed orally and is used only to treat gastrointestinal infections. After maternal use, rifamycin is unlikely to enter breast milk or the infant's bloodstream, and is unlikely to have any adverse effects on breastfed infants. ◉ Effects on Breastfed Infants As of the revision date, no relevant published information was found. ◉ Effects on Lactation and Breast Milk As of the revision date, no relevant published information was found. The toxicological profile of Rifamycin·Na is related to its antibacterial activity and effects on liver function. It interferes with hepatic bile acid metabolism. The compound is generally well-tolerated at therapeutic doses but may cause gastrointestinal disturbances. It is intended for research use and clinical applications require appropriate medical supervision. Comprehensive toxicity studies have been conducted to support its use as an antibiotic. |
| References | |
| Additional Infomation |
See also: Rifamycin sodium (preferred); Rifamycin (with active fraction).
Rifamycin·Na is a valuable research tool for studying bacterial transcription, antibiotic mechanisms, and tuberculosis. Its inhibition of bacterial RNA polymerase makes it useful for investigating the mechanism of transcription and for developing new antibiotics. Its activity against M. tuberculosis makes it relevant for tuberculosis research. The compound can be employed in studies on antibiotic resistance and combination therapy. It is also used as an analytical standard for the quality control of rifamycin antibiotics. |
| Molecular Formula |
C37H46NNAO12
|
|---|---|
| Molecular Weight |
719.8
|
| Exact Mass |
719.291
|
| CAS # |
14897-39-3
|
| Related CAS # |
Rifamycin; 6998-60-3
|
| PubChem CID |
42620466
|
| Appearance |
Light brown to brown solid
|
| Density |
1.35g/cm3
|
| Boiling Point |
862.1ºC at 760mmHg
|
| Melting Point |
>215°C (dec.)
|
| Flash Point |
475.2ºC
|
| LogP |
5.187
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
51
|
| Complexity |
1340
|
| Defined Atom Stereocenter Count |
9
|
| SMILES |
[Na+].O(C(C([H])([H])[H])=O)[C@]1([H])[C@]([H])(C([H])([H])[H])[C@]([H])(C([H])=C([H])O[C@]2(C([H])([H])[H])C(C3C4=C(C([H])=C(C(=C4C(=C(C([H])([H])[H])C=3O2)O[H])O[H])N([H])C(C(C([H])([H])[H])=C([H])C([H])=C([H])[C@]([H])(C([H])([H])[H])[C@@]([H])([C@@]([H])(C([H])([H])[H])[C@]([H])([C@@]1([H])C([H])([H])[H])O[H])O[H])=O)[O-])=O)OC([H])([H])[H] |c:18,62,t:58|
|
| InChi Key |
YVOFSHPIJOYKSH-NLYBMVFSSA-M
|
| InChi Code |
InChI=1S/C37H47NO12.Na/c1-16-11-10-12-17(2)36(46)38-23-15-24(40)26-27(32(23)44)31(43)21(6)34-28(26)35(45)37(8,50-34)48-14-13-25(47-9)18(3)33(49-22(7)39)20(5)30(42)19(4)29(16)41;/h10-16,18-20,25,29-30,33,40-44H,1-9H3,(H,38,46);/q;+1/p-1/b11-10+,14-13+,17-12-;/t16-,18+,19+,20+,25-,29-,30+,33+,37-;/m0./s1
|
| Chemical Name |
sodium;(7S,9E,11S,12R,13S,14R,15R,16R,17S,18S,19E,21Z)-13-acetyloxy-2,15,17,29-tetrahydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-6,23-dioxo-8,30-dioxa-24-azatetracyclo[23.3.1.14,7.05,28]triaconta-1(29),2,4,9,19,21,25,27-octaen-27-olate
|
| Synonyms |
Rifamycin SV monosodiumRifocin RifamasteneCB-0111, NSC146718 CB 01-11, NSC-146718
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~347.34 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (2.89 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3893 mL | 6.9464 mL | 13.8927 mL | |
| 5 mM | 0.2779 mL | 1.3893 mL | 2.7785 mL | |
| 10 mM | 0.1389 mL | 0.6946 mL | 1.3893 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04349579 | Active recruiting |
Drug: Rifamycine Drug: Saline Solution |
Impacted Third Molar Tooth | Yuzuncu Yıl University | November 15, 2018 | Phase 4 |
| NCT03345823 | Active recruiting |
Drug: Upadacitinib Drug: Placebo for Upadacitinib |
Crohn's Disease | AbbVie | March 21, 2018 | Phase 3 |
| NCT04026984 | Not yet recruiting | Drug: Rifamycin SV-MMX Drug: Placebo |
Traveler's Diarrhea | RedHill Biopharma Limited | June 2024 | Phase 2 |
| NCT04027894 | Not yet recruiting | Drug: Rifamycin SV MMX Drug: Placebo to Rifamycin SV-MMX |
Traveler's Diarrhea | RedHill Biopharma Limited | January 2024 | Phase 2 |
| NCT05588492 | Recruiting | Drug: Rifamycin-free regimen Drug: Rifamycin-containing regimen |
Pulmonology | National Taiwan University Hospital |
January 1, 2022 | Phase 4 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
