| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
The specific molecular targets of Antibiotic-5d are not well-defined in the available literature. As a synthetic antimicrobial compound, it is likely to target essential bacterial cellular processes, such as cell wall synthesis, protein synthesis, DNA replication, or membrane integrity. Its activity against both Gram-positive and Gram-negative bacteria suggests that it may target a conserved bacterial pathway or structure. Its activity against fungi and yeast further indicates a broad-spectrum mechanism that may involve targeting eukaryotic cell membrane components or other essential processes. Further studies are needed to identify its precise molecular target(s) and mechanism of action.
|
|---|---|
| ln Vitro |
Several Gram-positive (Staphylococcus aureus, Bacillus cereus, etc.) and Gram-negative (E. coli, Proteus vulgaris, etc.) bacteria, fungi, and yeast are susceptible to the effects of antibiotic-5d when cultured in vitro. Bacteria (yeast) also show modest antibacterial activity against various Gram-positive (Saccharomyces cerevisiae, etc.).
In vitro, Antibiotic-5d exhibits moderate antibacterial activity against various Gram-positive and Gram-negative bacteria. It is active against Staphylococcus aureus, Bacillus cereus, Escherichia coli, and Proteus vulgaris. It also shows activity against fungi such as Candida albicans and yeast such as Saccharomyces cerevisiae. The compound's antimicrobial activity is moderate, indicating that it may not be as potent as clinically used antibiotics but could serve as a lead compound for further optimization. Its broad-spectrum activity makes it a valuable tool for studying antimicrobial mechanisms and for screening against various microbial pathogens. In vitro studies typically involve determining the minimum inhibitory concentration (MIC) against a panel of microbial strains. |
| ln Vivo |
In vivo activity data for Antibiotic-5d are not well-documented in the available literature. As a synthetic antimicrobial compound with moderate in vitro activity, its in vivo efficacy would need to be evaluated in animal models of infection. Such studies would involve infecting animals (e.g., mice) with pathogenic bacteria and administering Antibiotic-5d via various routes (e.g., oral, intraperitoneal, or intravenous). The compound's ability to reduce bacterial load, improve survival, and resolve infection would be assessed. Pharmacokinetic and toxicity studies would also be required to determine its suitability for in vivo use. Further research is needed to evaluate its in vivo activity.
|
| Enzyme Assay |
The antimicrobial activity of Antibiotic-5d can be assessed using standard cell-free or whole-cell assays. A typical protocol for determining the minimum inhibitory concentration (MIC) involves preparing serial two-fold dilutions of the compound in a suitable medium (e.g., Mueller-Hinton broth). A standardized inoculum of the test microorganism is added to each well, and the plates are incubated at 37degC for 18-24 hours. The MIC is the lowest concentration of the compound that inhibits visible growth of the microorganism. The minimum bactericidal concentration (MBC) can be determined by subculturing aliquots from wells showing no growth onto agar plates and incubating for an additional 24 hours.
|
| Cell Assay |
For in vitro cellular experiments, microbial cultures (e.g., bacteria, fungi, yeast) are grown to logarithmic phase in appropriate media and diluted to a standard cell density. The cultures are then treated with Antibiotic-5d at various concentrations (typically 0.1-100 microg/mL) and incubated at the optimal growth temperature for the microorganism (e.g., 37degC for bacteria, 30degC for fungi). After incubation, cell viability is measured by plating serial dilutions onto agar plates and counting colony-forming units (CFUs). Alternatively, the optical density (OD600) of the culture can be measured to assess growth inhibition. The duration of treatment varies depending on the microorganism and the specific experimental objectives.
|
| Animal Protocol |
In vivo animal experiments with Antibiotic-5d would typically involve murine models of infection. A common protocol involves infecting mice with a lethal dose of a pathogenic bacterium (e.g., Staphylococcus aureus or Escherichia coli) via intraperitoneal or intravenous injection. Antibiotic-5d is then administered at various doses and routes (e.g., oral, intravenous, or intraperitoneal) either prophylactically or therapeutically. Survival is monitored for 7-14 days, and bacterial load in blood and tissues is measured at various time points by plating serial dilutions on agar plates. The compound's efficacy is assessed by comparing survival rates and bacterial clearance between treated and control groups.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for Antibiotic-5d are not well-documented in the available literature. As a research compound, its absorption, distribution, metabolism, and excretion properties have not been extensively characterized. Its molecular weight and chemical structure suggest that it may have moderate lipophilicity and could be orally bioavailable, but this has not been confirmed. Further studies are needed to determine its pharmacokinetic profile, including oral bioavailability, half-life, protein binding, and tissue distribution. These properties would be essential for evaluating its potential as a therapeutic agent.
|
| Toxicity/Toxicokinetics |
The toxicity profile of Antibiotic-5d has not been extensively characterized. As a synthetic antimicrobial compound, it may have potential toxicity to mammalian cells, particularly at high concentrations. Its moderate antimicrobial activity suggests that it may have a relatively narrow therapeutic window. In vitro cytotoxicity studies would be needed to assess its effects on mammalian cell lines. In vivo toxicity studies in animal models would also be required to determine its safety profile. The compound should be handled with standard laboratory precautions and is intended for research use only.
|
| References |
[1]. Stanchev M, et al. Synthesis and antimicrobial activity in vitro of new amino acids and peptides containing thiazole and oxazole moieties. Arch Pharm (Weinheim). 1999 Sep;332(9):297-304.
|
| Additional Infomation |
Antibiotic-5d is a synthetic antimicrobial compound with moderate broad-spectrum activity against Gram-positive and Gram-negative bacteria, fungi, and yeast. It is active against Staphylococcus aureus, Bacillus cereus, Escherichia coli, Proteus vulgaris, Candida albicans, and Saccharomyces cerevisiae. The compound is a research tool for studying antimicrobial mechanisms and for screening against various microbial pathogens. Its moderate activity and broad spectrum make it a useful lead compound for the development of new antibiotics. Antibiotic-5d is available as a research compound and is not approved for clinical use.
|
| Molecular Formula |
C13H18N2O4S
|
|---|---|
| Molecular Weight |
298.3580
|
| Exact Mass |
298.099
|
| CAS # |
251349-54-9
|
| Related CAS # |
251349-54-9;
|
| PubChem CID |
10709196
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.851
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
20
|
| Complexity |
396
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
S1C([H])=C(C(=O)O[H])N=C1[C@]1([H])C([H])([H])C([H])([H])C([H])([H])N1C(=O)OC(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H]
|
| InChi Key |
DPLVJSMBNOUIIM-VIFPVBQESA-N
|
| InChi Code |
InChI=1S/C13H18N2O4S/c1-13(2,3)19-12(18)15-6-4-5-9(15)10-14-8(7-20-10)11(16)17/h7,9H,4-6H2,1-3H3,(H,16,17)/t9-/m0/s1
|
| Chemical Name |
2-[(2S)-1-[(2-methylpropan-2-yl)oxycarbonyl]pyrrolidin-2-yl]-1,3-thiazole-4-carboxylic acid
|
| 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) |
DMSO : ~100 mg/mL (~335.17 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.38 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3517 mL | 16.7583 mL | 33.5166 mL | |
| 5 mM | 0.6703 mL | 3.3517 mL | 6.7033 mL | |
| 10 mM | 0.3352 mL | 1.6758 mL | 3.3517 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
