Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
TOPO IV 0.059 μM (IC50, E. coli ) TOPO IV 0.341 μM (IC50, S. aureus) DNA gyrase 0.185 μM (IC50, S. aureus) DNA gyrase 0.365 μM (IC50, E. coli )
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ln Vitro |
Compound 12, or anti-MRSA agent 7, exhibits a dose-dependent bactericidal efficacy at a dosage of 8 times MIC against free methicillin-resistant Staphylococcus aureus (ATCC 43300) within 8 hours of treatment, but regrowth afterwards[1]. Gram-positive and Gram-negative bacterial pathogens are the targets of Anti-MRSA agent 7 (Compound 12)'s antimicrobial activity[1]. ATCC 29213 strain of S. aureus N43 (CGSC# 5583) E. Coli MRSAQA-12.1 MRSA Q.A. -11.7 E. coli DRK 057 MRSA QA-11.2 E. faecalis (ATCC 25922) MIC(μM) 0.03 0.03 0.06 0.06 0.124 4.07 252 A. baumannii x E. coli strain D22 10.3 K. pneumoniae ESBL QA RDK 030c S. alachua P. aeruginosa RDK 184 MIC(μM) 252 252 >252 >252 >252 more than 252
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ln Vivo |
In the MRSA neutropenic mouse thigh infection model, anti-MRSA agent 7 (Compound 12; 20 and 40 mg/kg; ip; QID for 1 day) shown strong in vivo activity [1].
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Animal Protocol |
Animal/Disease Models: CD-1 female mice, MRSA neutropenic mouse thigh infection model[1]
Doses: 20 and 40 mg/kg Route of Administration: IP/QID (four times a day) at 2, 8, 14, and 20 h post infection Experimental Results: Demonstrated inhibition of bacterial growth in a dose dependent manner. |
References |
[1]. Kokot M, et al. Amide containing NBTI antibacterials with reduced hERG inhibition, retained antimicrobial activity against gram-positive bacteria and in vivo efficacy. Eur J Med Chem. 2023 Mar 15;250:115160.
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Molecular Formula |
C22H20BRF2N3O4
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Molecular Weight |
508.31
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9673 mL | 9.8365 mL | 19.6730 mL | |
5 mM | 0.3935 mL | 1.9673 mL | 3.9346 mL | |
10 mM | 0.1967 mL | 0.9837 mL | 1.9673 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.