| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Antimicrobial agent 330 (compound I-10b) can effectively inhibit the growth of a variety of Gram-positive and Gram-negative bacteria (MIC = 0.0007-0.0026 mM), with the lowest MIC against Enterococcus faecalis at 0.0003 mM, and can also inhibit clinically isolated Enterococcus faecalis strains at low concentrations [1]. Antimicrobial agent 330 (4-8 times MIC; action time up to 8 hours) showed concentration-dependent bactericidal activity against Staphylococcus aureus 25923 and Enterococcus faecalis, and at 8 times MIC concentration, colony-forming units (CFU) were significantly reduced within 6 hours [1]. Antimicrobial agent 330 (14 days) had a low probability of inducing drug resistance in Staphylococcus aureus 25923 and Enterococcus faecalis, and could effectively inhibit sulfamethoxazole-resistant strains at low concentrations (0.0007-0.0055 mM) [1]. The hemolytic toxicity of antimicrobial agent 330 (32-64 times MIC; 4 hours) is negligible [1]. Antimicrobial agent 330 (5-40 μg/mL) has no significant cytotoxicity to normal human hepatocytes LO2 and lung epithelial cells Beas-2b [1]. Antimicrobial agent 330 (0.5×-16×MIC) can effectively inhibit and clear the biofilm of Staphylococcus aureus 25923 and Enterococcus faecalis in a concentration-dependent manner, and the clearance rate of Staphylococcus aureus 25923 biofilm at a concentration of 16×MIC exceeds 40% [1]. Antimicrobial agent 330 (1×-16×MIC) can increase the membrane permeability of Staphylococcus aureus 25923 and Enterococcus faecalis [1]. Antimicrobial agent 330 (0.5×-8×MIC) can induce protein leakage of Staphylococcus aureus 25923 and Enterococcus faecalis in a concentration-dependent manner, indicating that the bacterial membrane is damaged [1]. Antimicrobial agent 330 (0.5×-16× MIC) can induce the accumulation of intracellular ROS in Staphylococcus aureus 25923 and Enterococcus faecalis in a concentration-dependent manner [1]. Antimicrobial agent 330 (4×-16× MIC) can inhibit the LDH activity of Staphylococcus aureus 25923 and Enterococcus faecalis by about 45% at 16× MIC [1].
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|---|---|
| ln Vivo |
Antibacterial agent 330 (compound I-10b) (0.007-0.014 mM; injection; single dose) has a strong antibacterial effect against Staphylococcus aureus 25923 in the larvae of the large wax moth. The 0.007 mM dose can achieve a 90% survival rate of larvae after 8 days, while the 0.014 mM dose can achieve almost complete survival of larvae [1]. Antibacterial agent 330 (4×MIC; topical application; once daily; for 6 consecutive days) can effectively promote wound healing and reduce the bacterial load of Staphylococcus aureus 25923 in a mouse wound infection model, while maintaining normal weight gain in mice [1]. Antibacterial agent 330 (5 mg/kg/day; once daily; for 3 consecutive days) showed good biocompatibility in Kunming mice, and no histopathological damage to major organs was observed [1].
|
| Animal Protocol |
Animal/Disease Models:Staphylococcus aureus 25923 infection of large wax moth larvae [1]
Doses: 0.007 mM (5× MIC); 0.014 mM (10× MIC)< Route of Administration:Injection; Single dose Experimental Experimental Results:The survival rate reached 90% 8 days after infection (0.007 mM dose). During the 8-day observation period, the survival rate was close to 100% (0.014 mM dose). The in vivo toxicity was low, and the survival rate was comparable to that of the saline control group. Animal/Disease Models:Staphylococcus aureus 25,923 Infected Mouse Wound Model (18-22 g, 3-8 weeks old) [1] Doses: 4×MIC Route of Administration:Topical application; once daily; for 6 days Experimental Results:Compared with the PBS and norfloxacin control groups, the residual bacterial load at the wound site was significantly reduced on day 6 after treatment. Compared with the norfloxacin group, the wound healing rate was faster, and the wound was almost completely closed on day 6. Weight gain was normal throughout the treatment period, consistent with the positive control group. |
| References |
| Molecular Formula |
C34H36CLN4O10PS
|
|---|---|
| Molecular Weight |
759.16
|
| CAS # |
3031427-16-1
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
CCOP(OCC)(C(C1=CC(OC)=C(C2=C[N+]3=C(C4=CC5=C(OCO5)C=C4CC3)C=C12)O)NC6=CC=C(C=C6)S(=O)(NC7=NOC(C)=C7)=O)=O.[Cl-]
|
| 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
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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 | 1.3172 mL | 6.5862 mL | 13.1725 mL | |
| 5 mM | 0.2634 mL | 1.3172 mL | 2.6345 mL | |
| 10 mM | 0.1317 mL | 0.6586 mL | 1.3172 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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