Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
Bacterial[1]
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ln Vitro |
Compound 23, or antibacterial agent 127, exhibited antibacterial activity against MRSA ATCC25923, MSSA ATCC29213, MRSAb, MRSEB, E. coli ATCC25922, and S. pullorum, with minimum inhibitory concentrations (MICs) of 0.063, 0.25, 32, and 64 μg/mL[1]. The metabolic stability of antibacterial agent 127 is good (t1/2 in rat liver microsomes is 3.25 min)[1]. With IC50 values of 2.64 and 1.94 μM, respectively, antibacterial agent 127 has a moderately inhibiting impact on CYP3A4 (midazolam) and CYP3A4 (testosterone) [1].
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ln Vivo |
In a mouse thigh infection model, antibacterial agent 127 (Compound 23) (50 mg/kg; ip; single dose) efficiently suppresses MRSA [1].
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Animal Protocol |
Animal/Disease Models: Female Kunming mice, neutropenic mouse thigh infection model[1]
Doses: 50 mg/kg Route of Administration: intraperitoneal (ip)injection, single dose Experimental Results: decreased bacteria count with a value of 1.84 log10 CFU/mL in comparison with vehicle control group. |
References |
[1]. Deng Y, et al. Antibacterial activity evaluation of pleuromutilin derivatives with 4(3H)-quinazolinone scaffold against methicillin-resistant Staphylococcusaureus. Eur J Med Chem. 2022 Nov 23;246:114960.
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Molecular Formula |
C28H37N3O5S
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Molecular Weight |
527.68
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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 | 1.8951 mL | 9.4754 mL | 18.9509 mL | |
5 mM | 0.3790 mL | 1.8951 mL | 3.7902 mL | |
10 mM | 0.1895 mL | 0.9475 mL | 1.8951 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.