| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
DuP 105 targets bacterial protein synthesis, a mechanism that distinguishes oxazolidinones from other classes of antibiotics. Unlike many other antibiotics that target the 30S ribosomal subunit, oxazolidinones bind to the 50S ribosomal subunit and inhibit the formation of the initiation complex during protein synthesis. This unique mechanism of action makes oxazolidinones effective against bacteria that are resistant to other antibiotic classes. DuP 105 has selective antibacterial activity against gram-positive bacteria, including staphylococci and streptococci. The compound does not show significant activity against gram-negative bacteria. Its activity against staphylococcal isolates has been demonstrated in vitro.
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| ln Vitro |
DuP 105 exhibits inhibitory activity against isolates of Bacteroides fragilis and Staphylococcus aureus, with MIC90s of 16 μg/mL and 4 to 16 μg/mL, respectively [1]. For half of the 216 Gram-positive isolates that were tested, the DuP 105 MIC (MIC50) varied from 4.0 to 16 μg/mL [2].
In vitro, DuP 105 has demonstrated inhibitory activity against staphylococcal isolates and other gram-positive bacteria. Its antibacterial activity is measured using standard broth microdilution or agar dilution methods, with MIC values determined against various gram-positive pathogens. The compound's unique mechanism of action, targeting the 50S ribosomal subunit, makes it effective against methicillin-resistant Staphylococcus aureus (MRSA) and other antibiotic-resistant strains. DuP 105 shows selective activity against gram-positive bacteria with minimal activity against gram-negative organisms. Its in vitro activity profile has been characterized in numerous studies since its discovery in the 1980s. |
| ln Vivo |
At 50% effective doses of 9 to 23 mg/kg, DuP 105 given orally or parenterally prevents streptococcal and staphylococcal infections in mice [1].
In vivo, DuP 105 has demonstrated protective effects in animal models of infection caused by gram-positive bacteria. The compound is orally active, making it suitable for oral administration in research settings. Its efficacy has been demonstrated in models of staphylococcal and streptococcal infections. However, the compound's development was discontinued in favor of other oxazolidinones, and detailed in vivo efficacy data are limited in the public literature. |
| Enzyme Assay |
For in vitro antibacterial susceptibility testing, standard procedures recommended by the CLSI are followed. Gram-positive bacterial strains (e.g., Staphylococcus aureus, Streptococcus pneumoniae, Enterococcus faecalis) are cultured on appropriate agar media and suspended to 0.5 McFarland standard. The bacterial suspension is inoculated onto Mueller-Hinton agar plates or into broth containing serial two-fold dilutions of DuP 105 (typically ranging from 0.015 to 256 μg/mL). After incubation at 35-37°C for 16-24 hours, the MIC is determined as the lowest concentration that inhibits visible bacterial growth. For quality control, reference strains with known MIC ranges are included. Time-kill curve assays are performed to evaluate bactericidal activity.
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| Cell Assay |
For in vitro cell-based assays, the antibacterial activity of DuP 105 can be evaluated using cell culture models of infection. Mammalian cell lines are cultured and infected with bacterial pathogens in the presence of varying concentrations of the compound. After incubation, bacterial counts are determined by plating serial dilutions. Cytotoxicity of the compound to mammalian cells is assessed using MTT or LDH release assays. The compound's effects on bacterial adhesion and invasion into host cells can also be studied.
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| Animal Protocol |
For in vivo animal studies, DuP 105 is typically administered orally or intraperitoneally in models of gram-positive bacterial infection. Mice or rats are infected with bacterial pathogens (e.g., Staphylococcus aureus, Streptococcus pneumoniae) via intravenous, intraperitoneal, or intranasal routes. The compound is administered at various doses and schedules, and survival, bacterial burden in tissues, and clinical signs are assessed. Pharmacokinetic studies may also be performed to determine drug concentrations in plasma and tissues.
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| ADME/Pharmacokinetics |
DuP 105 is orally bioavailable. As a small molecule with a molecular weight of 296.34, it is expected to be well absorbed from the gastrointestinal tract. The compound is metabolized in the liver, and its metabolites may be excreted in urine and feces. Detailed pharmacokinetic parameters, including Cmax, Tmax, half-life, and bioavailability, have not been extensively characterized in the public literature. The compound's solubility and formulation for oral administration have been described.
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| Toxicity/Toxicokinetics |
Specific toxicity data for DuP 105 are limited. As an investigational antibacterial agent, the compound has been evaluated in preclinical safety studies. However, comprehensive toxicological data have not been published. The compound should be handled with standard laboratory safety precautions. It is not intended for human use and is for research purposes only.
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| References |
[1]. Slee AM, et al. Oxazolidinones, a new class of synthetic antibacterial agents: in vitro and in vivo activities of DuP 105 and DuP 721. Antimicrob Agents Chemother. 1987 Nov;31(11):1791-7.
[2]. Barry AL, et al. In vitro evaluation of DuP 105 and DuP 721, two new oxazolidinone antimicrobial agents. Antimicrob Agents Chemother. 1988 Jan;32(1):150-2 |
| Additional Infomation |
DuP 105 is a research compound with no clinical trial or regulatory approval status. It is a member of the oxazolidinone class of antibacterial agents, which was first discovered in the 1980s. Although DuP 105 itself did not advance to clinical development, its discovery paved the way for the development of later oxazolidinone antibiotics, including linezolid (Zyvox), which became the first FDA-approved oxazolidinone in 2000. DuP 105 is used primarily as a research tool in antibacterial drug discovery and as a reference standard for analytical method development. The compound is commercially available from chemical suppliers for research purposes only.
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| Molecular Formula |
C13H16N2O4S
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|---|---|
| Molecular Weight |
296.34214
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| Exact Mass |
296.083
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| CAS # |
96800-41-8
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| PubChem CID |
57141
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| Appearance |
White to off-white solid powder
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| LogP |
2.206
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
407
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(NC[C@H]1CN(C2=CC=C(S(C)=O)C=C2)C(O1)=O)=O
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| InChi Key |
RYTTWOVTZKVWTO-ZOZMEPSFSA-N
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| InChi Code |
InChI=1S/C13H16N2O4S/c1-9(16)14-7-11-8-15(13(17)19-11)10-3-5-12(6-4-10)20(2)18/h3-6,11H,7-8H2,1-2H3,(H,14,16)/t11-,20?/m0/s1
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| Chemical Name |
N-[[(5S)-3-(4-methylsulfinylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: ~125 mg/mL (~421.8 mM; with ultrasonication)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3745 mL | 16.8725 mL | 33.7450 mL | |
| 5 mM | 0.6749 mL | 3.3745 mL | 6.7490 mL | |
| 10 mM | 0.3375 mL | 1.6873 mL | 3.3745 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.
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