Rifalazil
Based on 1 Customer Validation
Rifalazil (KRM-1648; ABI-1648), a rifamycin derivative, inhibits the bacterial DNA-dependent RNA polymerase and kills bacterial cells by blocking off the β-subunit in RNA polymerase. Rifalazil (KRM-1648; ABI-1648) is an antibiotic, exhibits high potency against mycobacteria, gram-positive bacteria, Helicobacter pylori, C. pneumoniae and C. trachomatis with MIC values from 0.00025 to 0.0025 μg/ml. Rifalazil (KRM-1648; ABI-1648) has the potential for the treatment of Chlamydia infection, Clostridium difficile associated diarrhea (CDAD), and tuberculosis (TB).
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- Purity: 99.64%
- CAS No.: 129791-92-0
- 화학식: C51H64N4O13
- 분자량:941.07
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
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- References
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Biological Activity
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RNA Polymerase |
Rifalazil exhibits antimicrobal activity against Gram-positive enteric bacteria, inhibits Clostridium difficile, Clostridium perfringens, Bacteroides fragilis with MIC50 value of 0.0015, 0.0039, 0.0313 μg/ml, respectively[3]. Rifalazil exhibits antimicrobal activity against Gram-negative enteric bacteria, inhibits Escherichia coli and Klebsiella pneumoniae with MIC50 value of 16 and 16 μg/ml, respectively[3]. Rifalazil exhibits antimicrobal activity against non-enteric Gram-positive bacteria, inhibits Methicillin-susceptible Staphylococcus aureus, Methicillin-resistant S. aureus, Methicillin- and quinolone-resistant S. aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Streptococcus pneumoniae with MIC50 value of 0.0078, 0.0078, 0.0078, 0.0078, 0.0002, 0.0001 μg/ml, respectively[3]. Rifalazil exhibits antimicrobal activity against Helicobacter pylori, Chlamydia pneumoniae and Chlamydia trachomatis with MIC50 value of 0.004, 0.000125 and 0.00025 μg/ml, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female CD-1 mice infected with 5.2 × 107 viable mycobacteria[2]
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Dosage:20, 25, and 150 mg/kg; 6-8 weeks
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Administration:Oral gavage
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Result:Combined with isoniazid (INH) showed its potential for short-course treatment of Mycobacterium tuberculosis infection.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 129791-92-0
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Appearance Solid
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분자량 941.07
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화학식 C51H64N4O13
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Color Blue to dark blue
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SMILES
CC(C)CN(CC1)CCN1C2=CC(O3)=C(C(O)=C2)N=C(C3=C(NC(/C(C)=C\C=C\[C@@H]([C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@@H]([C@@H]([C@H](/C=C/O[C@@]4(C)O5)OC)C)OC(C)=O)C)=O)C6=O)C7=C6C(O)=C(C)C5=C7C4=O
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Synonyms
KRM-1648; ABI-1648
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
DMSO : 8.33 mg/mL (8.85 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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: ≥ 2.2 mg/mL (2.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.0 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: ≥ 2.2 mg/mL (2.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
순도&문서
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Data Sheet (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Suchland RJ, et al. Rifalazil pretreatment of mammalian cell cultures prevents subsequent Chlamydia infection.Antimicrob Agents Chemother. 2006 Feb;50(2):439-44. [Content Brief]
[2]. Shoen CM, et al. Evaluation of rifalazil in long-term treatment regimens for tuberculosis in mice.Antimicrob Agents Chemother. 2000 Jun;44(6):1458-62. [Content Brief]
[3]. Rothstein DM, et al. Development potential of rifalazil.Expert Opin Investig Drugs. 2003 Feb;12(2):255-71. [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 (sealed storage, away from moisture). 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 | 1.0626 mL | 5.3131 mL | 10.6262 mL | 26.5655 mL |
| 5 mM | 0.2125 mL | 1.0626 mL | 2.1252 mL | 5.3131 mL |
Rifalazil Related Classifications
HY-105099 Related Classifications
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