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250mg |
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500mg |
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1g |
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2g |
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5g |
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10g |
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25g |
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Enoxacin (also known as AT-2266, CI919, Pd107779, NSC 629661) is an orally bioavailable, broad-spectrum antibacterial agent of the fluoroquinolone class. It is used to treat a wide range of infections, including gonorrhea and urinary tract infections, by inhibiting bacterial DNA gyrase and topoisomerase IV. By binding to the DNA active site, enoxacin modifies the enzyme's breakage/reunion activity. In the absence of ATP, enoxacin promotes the cleavage of both relaxed and supercoiled forms of DNA.
Targets |
Quinolone
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ln Vitro |
Enoxacin hydrate (also known as Enoxacin sesquihydrate) improves in a dose-dependent manner, with a median effective concentration (EC50) of approximately 30 µM, siGFP-mediated gene knockdown mediated by siRNA against EGFP in HEK293 cells-based reporter system, while having no effect on the cells expressing GFP alone. In HEK293 cells, enoxacin (50 µM) facilitates siRNA duplex loading onto RISCs and miRNA processing[3].
Enoxacin has no impact on the way that Dicer alone processes pre-let-7 or pre-miR-30a. On the other hand, the combination of Enoxacin and TRBP can improve let-7 or pre-miR-30a processing[3]. Enoxacin inhibits 90% of the following microorganisms: Escherichia coli, Aeromonas sp., Enterobacter spp., Serratia spp., Proteus mirabilis, and Morganella morganii at less than or equal to 0.8 micrograms/ml[5]. |
ln Vivo |
Enoxacin hydrate (Enoxacin sesquihydrate; 100 µM; 2 µl; injected into ear once a day for 3 consecutive days (days 12, 13 and 14)) improves the efficiency of Lv-siGFP-induced GFP mRNA knockdown (from 80% to 60%; 40% GFP mRNA level remained), while alone has no effect on GFP expression in the GFP transgenic line C57BL/6-Tg(ACTB-EGFP)1Osb/J (10 d old) using lentivirus expressing shGFP (Lv-siGFP; injected into ear for 10 days)[3].
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References |
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Molecular Formula |
C₁₅H₁₇FN₄O₃.₃/₂H₂O
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Molecular Weight |
347.34
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CAS # |
84294-96-2
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Related CAS # |
84294-96-2 (Enoxacin hydrate;Enoxacin sesquihydrate; AT-2266 hydrate; CI-919 hydrate); 74011-58-8 (free)
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Appearance |
Powder
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SMILES |
O=C(C1=CN(CC)C2=C(C=C(F)C(N3CCNCC3)=N2)C1=O)O.[1.5H2O]
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Synonyms |
Enoxacin sesquihydrate; AT-2266 hydrate; CI-919 hydrate; Enoxacin hydrate
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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) |
1M NaOH: ~100 mg/mL (~287.9 mM)
DMSO: ~2.78 mg/mL (~8.0 mM) H2O: ~1 mg/mL (~2.9 mM) |
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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 | 2.8790 mL | 14.3951 mL | 28.7902 mL | |
5 mM | 0.5758 mL | 2.8790 mL | 5.7580 mL | |
10 mM | 0.2879 mL | 1.4395 mL | 2.8790 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.
Enoxacin potentiates additional synthetic siRNA-induced gene knockdown. Nat Biotechnol . 2008 Aug;26(8):933-40. td> |
Enoxacin promotes the processing of miRNAs and the loading of siRNA duplexes onto RISCs. Nat Biotechnol . 2008 Aug;26(8):933-40. td> |
Enoxacin facilitates the TRBP-RNA interaction, and the RNAi-enhancing activity is TRBP-dependent. Nat Biotechnol . 2008 Aug;26(8):933-40. td> |
Enoxacin treatment has cancer-specific inhibitory effect. Proc Natl Acad Sci U S A . 2011 Mar 15;108(11):4394-9. td> |
Enoxacin enhances miRNA production through binding to TRBP protein. Proc Natl Acad Sci U S A . 2011 Mar 15;108(11):4394-9. td> |
Enoxacin growth-inhibitory and miRNA-enhancing expression is TRBP-dependent. Proc Natl Acad Sci U S A . 2011 Mar 15;108(11):4394-9. td> |