Size | Price | |
---|---|---|
100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
Target: Filamenting temperature-sensitive mutant Z (FtsZ)[1]
|
---|---|
ln Vitro |
Minimum bactericidal concentration (MBC) is the same as minimum inhibition concentration (MIC). Compound 30, FtsZ-IN-4, demonstrates strong antibacterial activity against S. aureus and B. subtilis, with MICs of 0.008–0.25 μg/mL, respectively[1]. The bactericidal effects of FtsZ-IN-4 (0.064 μg/mL or 0.5 μg/mL; 0-24 h) are demonstrated within 3 hours, and the MBC/MIC ratios are ≤4, meeting CLSI standards[1]. FtsZ-IN-4 exhibits minimal cytotoxicity against Vero cells (>20 μg/mL; 72 h) [1]. Bacteria are lengthened by FtsZ-IN-4 (0.016 μg/mL; 3 h), which also induces aberrant bacterial cell division and ultimately results in bacterial cell death[1]. SaFtsZ polymerization is induced by FtsZ-IN-4 (10 μg/mL; 0–15 min), and SaFtsZ GTPase activity is dose-dependently inhibited by FtsZ-IN-4 (0–35 μg/mL; 30 min)[1].
|
ln Vivo |
FtsZ-IN-4 (compound 30) (5 mg/kg; po) in mice shows a moderate exposure (AUC(0-t) = 544.2 h*ng/mL) and 61.2% oral bioavailability (F)[1]. Mice treated with FtsZ-IN-4 (25 mg/kg; iv) exhibit good in vivo effectiveness. The pharmacokinetic profiles of FtsZ-IN-4 in mice were as follows: Route Dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUC(0-t) (h·ng/mL) AUC(0-∞) (h·ng/mL) Vss (ng/mL) CL (mL/h/kg) F (%) iv 1 0.28 0.083 480.5 177.8 178.7 1545.5 5682.8 / 5 2.26 0.5 429.3 544.2 559.3 / / 61.2
|
Cell Assay |
Cell Cytotoxicity Assay[1]
Cell Types: Vero cells (African green monkey kidney cells) Tested Concentrations: >20 μg/mL Incubation Duration: 72 hrs (hours) Experimental Results: demonstrated the 50% cytotoxic concentration (CC50) >20 μg/ mL, much more than the inhibition of B. subtilis ATCC9372 (MIC =0.016 μg/mL). Cell Proliferation Assay[1] Cell Types: S. aureus ATCC25923 and Bacillus ATCC9372 Tested Concentrations: 1×, 2×, 4×, 8× MIC; MIC =0.125 μg/mL (S. aureus); 0.016 μg/mL (Bacillus) Incubation Duration: 3, 6, 12, 24 hrs (hours) Experimental Results: diminished B. subtilis ATCC9372 and S. aureus ATCC25923 cells below the lowest detectable limit (103 CFU/mL) in 3 h. |
Animal Protocol |
Animal/Disease Models: Male ICR mice (infected with S. aureus ATCC25923)[1]
Doses: 25 mg/ kg Route of Administration: intraperitoneal (ip) injection; 0.5 mL Experimental Results: Dramatically decreased the bacterial burden and demonstrated comparable in vivo efficacy with vancomycin. |
References |
[1]. Deng J, et al. Design, synthesis and biological evaluation of biphenyl-benzamides as potent FtsZ inhibitors. Eur J Med Chem. 2022 Sep 5. 239:114553.
|
Molecular Formula |
C21H16CLF2NO2
|
---|---|
Molecular Weight |
387.81
|
CAS # |
2882904-64-3
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
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 |
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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
---|---|
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.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5786 mL | 12.8929 mL | 25.7858 mL | |
5 mM | 0.5157 mL | 2.5786 mL | 5.1572 mL | |
10 mM | 0.2579 mL | 1.2893 mL | 2.5786 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.