| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
ATM enhancer-1 (compound 9) (0.1, 1, 10, 70 μM; 20 min) inhibited purified β-lactamases KPC-2, NDM-1, VIM-2, OXA-48, and OXA-10 with IC50 values ranging from 1.6 to 26.7 μM, with the strongest inhibitory activity against NDM-1 [1]. ATM enhancer-1 (0, 10, 25, 50 μM; 10 min) bound to the active site of purified NDM-1, exhibiting concentration-dependent quenching of tryptophan intrinsic fluorescence [1]. ATM enhancer-1 (8 mg/L; 60 min) inhibited the efflux pump in NDM-1-producing Pseudomonas aeruginosa strain PA-017, exhibiting enhanced intracellular retention of ethidium bromide [1]. ATM synergist-1 (16 mg/L; 24 hours) enhanced the activity of aztreonam against NDM-1-producing Pseudomonas aeruginosa PA-017 strain, reducing the MIC of aztreonam from 16 mg/L to 1 mg/L [1]. ATM synergist-1 (1, 2, 4, 8, 16, 32 mg/L; 18-24 hours) enhanced the activity of aztreonam against 29 carbapenemase-producing carbapenem-resistant Pseudomonas aeruginosa isolates, with 93% of the isolates showing synergistic effects (FICI ≤0.5), and the MIC of aztreonam decreasing by ≥4-fold [1]. ATM synergist-1 (1, 2, 4, 8, 16, 32 mg/L) did not increase the outer membrane permeability of NDM-1-producing Pseudomonas aeruginosa PA-017 strain, and the NPN fluorescence intensity remained unchanged [1]. ATM enhancer-1 (0.5, 1, 2, 4, 8, 16, 32 mg/L; 24 h) did not reduce the viability of immortalized human embryonic kidney HEK293 cells after 24 hours of incubation [1]. ATM enhancer-1 (4, 8, 16, 32 mg/L; 30 min) did not cause hemolysis of human erythrocytes after incubation at 37 °C for 30 minutes [1].
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|---|---|
| ln Vivo |
ATM enhancer-1 (compound 9) (40 mg/kg; intraperitoneal injection; 4 times every 2 hours, in combination with 20 mg/kg aztreonam) reduced bacterial load by 3.4 log10 in a mouse model of infection of NDM-1-producing Pseudomonas aeruginosa in the thigh[1]. ATM enhancer-1 (10-40 mg/kg; intraperitoneal injection; single dose) was well tolerated in 6-week-old female C57BL/6J mice with a 100% survival rate within 7 days[1].
|
| Cell Assay |
Cytotoxicity assay [1]
Cell Types: Immortalized human embryonic kidney cells (HEK293) Concentration: 0.5, 1, 2, 4, 8, 16, 32 mg/L Incubation Duration: 24 hours Experimental Results: Concentrations up to 32 mg/L did not affect the viability of HEK293 cells. |
| Animal Protocol |
Animal/Disease Models:C57BL/6J mice (7-week-old females, 20-22 g, infected with NDM-1-producing Pseudomonas aeruginosa strain PA-017 via intramuscular injection in the thigh) [1]
Doses: 40 mg/kg (in combination with 20 mg/kg aztreonam) Route of Administration: Intraperitoneal injection; once every 2 hours for a total of 4 times Experimental Results: The mean bacterial load in the thigh tissue decreased to 4.26 log10 CFU/thigh, a decrease of 3.4 log10 compared with the untreated control group. The reduction effect was better than that of aztreonam alone (a decrease of 2.2 log10). The thigh muscle weight decreased by 26.4% compared with the untreated control group. No significant changes in body weight or obvious clinical symptoms were observed. Animal/Disease Models:C57BL/6J mice (6-week-old females)[1] Doses: 10 mg/kg; 20 mg/kg; 40 mg/kg Route of Administration: Intraperitoneal injection; Single dose Experimental Results: The survival rate of mice in all dosage groups was 100% during the 7-day observation period. |
| References |
| Molecular Formula |
C23H22F2N4O5
|
|---|---|
| Molecular Weight |
472.44
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
OC1=C2C(C(OCCC(C)(C)C)=C(OC2=CC(OCC3=NN=NN3)=C1)C4=CC=C(C(F)=C4)F)=O
|
| 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) |
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 | 2.1167 mL | 10.5834 mL | 21.1667 mL | |
| 5 mM | 0.4233 mL | 2.1167 mL | 4.2333 mL | |
| 10 mM | 0.2117 mL | 1.0583 mL | 2.1167 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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