Garenoxacin Mesylate hydrate
Based on 1 Customer Validation
Garenoxacin (BMS284756) Mesylate hydrate is an orally active quinolone antibiotic and has a broad spectrum of activity against a wide array of gram-positive and gram-negative bacteria, anaerobes, and fastidious organisms.
For research use only. We do not sell to patients.
- Purity: 99.95%
- CAS No.: 223652-90-2
- Formula: C24H26F2N2O8S
- Molecular Weight:540.53
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Quinolone |
Gyrase 1.25 μg/mL (IC50) |
TOPO IV 1.5-2.5 μg/mL (IC50) |
Garenoxacin (BMS284756) (0-8 days) inhibits mycoplasmas and ureaplasmas with MIC90s ≤0.25 μg/mL against tested strains[1].
Garenoxacin (48 h) inhibits S. aureus wild type and mutants with MICs of 0.0128-4.0 μg/mL[2].
Garenoxacin inhibits topoisomerase IV and gyrase from S. aureus with IC50s of 1.25 to 2.5 and 1.25 μg/mL, respectively[2].
Garenoxacin has a low propensity for selective enrichment of fluoroquinolone-resistant mutants among ciprofloxacin-susceptible isolates of S. aureus[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:M. pneumonia, M. fermentans, M. hominis and Ureaplasma spp.
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Concentration:
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Incubation Time:24 h for Ureaplasma spp., 48 h for M. hominis, 4 to 8 days for M. pneumonia
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Result:Showed inhibition with MIC90s of 0.031 μg/mL, ≤0.008 μg/mL, ≤0.008 μg/mL and 0.25 μg/mL against M. pneumonia, M. fermentans, M. hominis and Ureaplasma spp. strains, respectively.
Garenoxacin (10 and 30 mg/kg; p.o.; once) reduces the viable cell counts in the lungs and significantly prolongs survival on experimental secondary pneumococcal pneumonia caused by S. pneumoniae D-979 in BALB/c female mice[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss mice with S. pneumonia infection[4].
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Dosage:12.5, 25 and 50 mg/kg
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Administration:Subcutaneous injection, once
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Result:Significantly improved the survival rate.
Chemical Information
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CAS No. 223652-90-2
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Appearance Solid
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Molecular Weight 540.53
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Formula C24H26F2N2O8S
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Color Off-white to gray
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SMILES
O=C(C1=CN(C2CC2)C3=C(C=CC(C4=CC5=C([C@@H](C)NC5)C=C4)=C3OC(F)F)C1=O)O.CS(=O)(O)=O.O
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Synonyms
BMS284756 Mesylate hydrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (185.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 12.5 mg/mL (23.13 mM; Need ultrasonic)
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.63 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Purity & Documentation
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Data Sheet (279 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]. Waites KB, et al. In vitro susceptibilities to and bactericidal activities of garenoxacin (BMS-284756) and other antimicrobial agents against human mycoplasmas and ureaplasmas. Antimicrob Agents Chemother. 2003 Jan;47(1):161-5. [Content Brief]
[2]. Ince D, et al. Dual targeting of DNA gyrase and topoisomerase IV: target interactions of garenoxacin (BMS-284756, T-3811ME), a new desfluoroquinolone. Antimicrob Agents Chemother. 2002 Nov;46(11):3370-80. [Content Brief]
[3]. Zhao X, et al. Mutant prevention concentration of garenoxacin (BMS-284756) for ciprofloxacin-susceptible or -resistant Staphylococcus aureus. Antimicrob Agents Chemother. 2003 Mar;47(3):1023-7. [Content Brief]
[4]. Azoulay-Dupuis E, et al. Activities of garenoxacin against quinolone-resistant Streptococcus pneumoniae strains in vitro and in a mouse pneumonia model. Antimicrob Agents Chemother. 2004 Mar;48(3):765-73. [Content Brief]
[5]. Fukuda Y, et al. Therapeutic effects of garenoxacin in murine experimental secondary pneumonia by Streptococcus pneumoniae after influenza virus infection. Diagn Microbiol Infect Dis. 2014 Feb;78(2):168-71. [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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.8500 mL | 9.2502 mL | 18.5004 mL | 46.2509 mL |
| 5 mM | 0.3700 mL | 1.8500 mL | 3.7001 mL | 9.2502 mL | |
| 10 mM | 0.1850 mL | 0.9250 mL | 1.8500 mL | 4.6251 mL | |
| 15 mM | 0.1233 mL | 0.6167 mL | 1.2334 mL | 3.0834 mL | |
| 20 mM | 0.0925 mL | 0.4625 mL | 0.9250 mL | 2.3125 mL | |
| DMSO | 25 mM | 0.0740 mL | 0.3700 mL | 0.7400 mL | 1.8500 mL |
| 30 mM | 0.0617 mL | 0.3083 mL | 0.6167 mL | 1.5417 mL | |
| 40 mM | 0.0463 mL | 0.2313 mL | 0.4625 mL | 1.1563 mL | |
| 50 mM | 0.0370 mL | 0.1850 mL | 0.3700 mL | 0.9250 mL | |
| 60 mM | 0.0308 mL | 0.1542 mL | 0.3083 mL | 0.7708 mL | |
| 80 mM | 0.0231 mL | 0.1156 mL | 0.2313 mL | 0.5781 mL | |
| 100 mM | 0.0185 mL | 0.0925 mL | 0.1850 mL | 0.4625 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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