| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
EC50: 1.4 μM (SaClpP)[1] Kd: 5.0 μM (SaClpP)[1]
|
|---|---|
| ln Vitro |
The melting point (Tm) of SaClpP was raised by (S)-ZG197 (10 μM; 2 h), but the Tm of HsClpP was hardly affected. The thermal stability of SaClpP is markedly enhanced by (S)-ZG197 [1]. The α-casein hydrolytic activity of the SaClpPI91W mutant is greatly reduced by (S)-ZG197 (0.1-100 μM; 2 h) [1]. When staphylococcal cells are intact, (S)-ZG197 (10 μM; 2 h) is unable to cause the Tm shift of SaClpPI91W [1]. At a MIC of 4 μg/mL, (S)-ZG197 (0-256 μg/mL; 18 h) inhibits the growth of Staphylococcus aureus 8325-4. With a minimum inhibitory concentration (MIC) of 2–8 μg/mL, (S)-ZG197 demonstrates potent and broad-spectrum antibacterial action against S. aureus[1]. In S. aureus 8325-4, (S)-ZG197 (0–20 μM) decreases the abundance of SaFtsZ, but has no effect on the ΔclpP mutant strain [1].
|
| ln Vivo |
The (S)-ZG197 (25-100 mg/kg; ip; once) considerably increases the zebrafish USA300 infection model's survival rate [1]. In a mouse skin S. aureus infection model, (S)-ZG197 (7.5 mg/kg; sc; twice daily for 3 days) demonstrates anti-infectious efficacy [1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: Cell lysates of S. aureus 8325-4 clpP knockout(ΔclpP) strain Tested Concentrations: 0, 2.5, 5 and 10 μM Incubation Duration: 15 min Experimental Results: SaFtsZ protein was degraded when SaClpP was added . |
| Animal Protocol |
Animal/Disease Models: Zebrafish USA300 infection model[1]
Doses: 25, 50, or 100 mg/kg Route of Administration: intraperitoneal (ip)injection, single dose Experimental Results: Dramatically prolong the survival rate at 50 mg/kg. Lost therapeutic effects on zebrafish infected with the ΔclpP mutant strain. Animal/Disease Models: Female balb/c (Bagg ALBino) mouse, S. aureus infection model[1] Doses: 7.5 mg/kg Route of Administration: subcutaneous (sc) injection, twice a day for 3 days Experimental Results: Caused a smaller necrotic lesion size in mice compared with the vehicle control. |
| References |
| Molecular Formula |
C28H35F3N4O3
|
|---|---|
| Molecular Weight |
532.6
|
| CAS # |
2999672-66-9
|
| Appearance |
Typically exists as solid 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 | 1.8776 mL | 9.3879 mL | 18.7758 mL | |
| 5 mM | 0.3755 mL | 1.8776 mL | 3.7552 mL | |
| 10 mM | 0.1878 mL | 0.9388 mL | 1.8776 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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