Enoxacin (AT-2266)

Alias: AT-2266; CI-919; NSC-629661; AT 2266; CI 919; NSC 629661; AT2266; CI919; NSC629661; PD-107779; Enoxacin; Penetrex; Enoxacine; Comprecin; Enoxacino; PD 107779; PD107779; Penetrex
Cat No.:V1405 Purity: ≥98%
Enoxacin (formerly AT-2266; CI-919; NSC-629661;Penetrex; Comprecin; Enoxacino)is an orally bioavailable and broad-spectrum fluoroquinolone antibiotic used to treat various infections, such as UTIs-urinary tract infections and gonorrhea.
Enoxacin (AT-2266) Chemical Structure CAS No.: 74011-58-8
Product category: Topoisomerase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
250mg
500mg
1g
2g
5g
10g
Other Sizes

Other Forms of Enoxacin (AT-2266):

  • Enoxacin hydrate (CI-919)
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Enoxacin (formerly AT-2266; CI-919; NSC-629661; Penetrex; Comprecin; Enoxacino) is an orally bioavailable and broad-spectrum fluoroquinolone antibiotic used to treat various infections, such as UTIs-urinary tract infections and gonorrhea. IIt acts by blocking topoisomerase IV and bacterial DNA gyrase.

Biological Activity I Assay Protocols (From Reference)
Targets
Topoisomerase II; Topoisomerase IV
ln Vitro

In vitro activity: Enoxacin (AT 2266) has no effect on cells expressing GFP alone, but it increases siGFP-mediated gene knockdown mediated by siRNA against EGFP in HEK293 cells-based reporter system in a dose-dependent manner, with a median effective concentration (EC50) of ~30 µM. 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 and TRBP can improve let-7 or pre-miR-30a processing[3]. 90% of Escherichia coli, Aeromonas, Enterobacter, Serratia, Proteus mirabilis, and Morganella morganii are inhibited by enoxacin at concentrations of less than or equal to 0.8 micrograms/ml[5].

ln Vivo
Enoxacin (AT 2266; 100 µM; 2 µl; injected into ear once a day for 3 consecutive days (days 12, 13 and 14)) increases Lv-siGFP'sabilityto knock down GFP mRNA (from 80% to 60%; 40% of GFP mRNA level remained); however, 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) alone has no effect on GFP expression[3].
Animal Protocol


References

[1]. Small molecule enoxacin is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2-mediated microRNA processing. Proc Natl Acad Sci U S A. 2011 Mar 15;108(11):4394-9.

[2]. Target preference of 15 quinolones against Staphylococcus aureus, based on antibacterial activities and target inhibition. Antimicrob Agents Chemother. 2001 Dec;45(12):3544-7.

[3]. A small molecule enhances RNA interference and promotes microRNA processing. Nat Biotechnol. 2008 Aug;26(8):933-40.

[4]. Small molecules with big roles in microRNA chemical biology and microRNA-targeted therapeutics. RNA Biol. 2019 Jun;16(6):707-718.

[5]. In vitro activity of enoxacin, a quinolone carboxylic acid, compared with those of norfloxacin, new beta-lactams, aminoglycosides, and trimethoprim. Antimicrobial agents and chemotherapy, 1983. 24(5): p. 754-763.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C15H17FN4O3
Molecular Weight
320.32
Exact Mass
320.13
Elemental Analysis
C, 56.24; H, 5.35; F, 5.93; N, 17.49; O, 14.98
CAS #
74011-58-8
Related CAS #
84294-96-2
Appearance
Solid powder
SMILES
CCN1C=C(C(=O)C2=CC(=C(N=C21)N3CCNCC3)F)C(=O)O
InChi Key
IDYZIJYBMGIQMJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H17FN4O3/c1-2-19-8-10(15(22)23)12(21)9-7-11(16)14(18-13(9)19)20-5-3-17-4-6-20/h7-8,17H,2-6H2,1H3,(H,22,23)
Chemical Name
1-ethyl-6-fluoro-4-oxo-7-piperazin-1-yl-1,8-naphthyridine-3-carboxylic acid
Synonyms
AT-2266; CI-919; NSC-629661; AT 2266; CI 919; NSC 629661; AT2266; CI919; NSC629661; PD-107779; Enoxacin; Penetrex; Enoxacine; Comprecin; Enoxacino; PD 107779; PD107779; Penetrex
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 Data
Solubility (In Vitro)
DMSO: ~32 mg/mL (~99.9 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.1219 mL 15.6094 mL 31.2188 mL
5 mM 0.6244 mL 3.1219 mL 6.2438 mL
10 mM 0.3122 mL 1.5609 mL 3.1219 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

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.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04840823 Active
Recruiting
Drug: Enoxacin
Drug: Placebo
Amyotrophic Lateral Sclerosis McGill University March 26, 2021 Phase 1
Phase 2
Biological Data
  • Enoxacin potentiates additional synthetic siRNA-induced gene knockdown. Nat Biotechnol . 2008 Aug;26(8):933-40.
  • Enoxacin promotes the processing of miRNAs and the loading of siRNA duplexes onto RISCs. Nat Biotechnol . 2008 Aug;26(8):933-40.
  • Enoxacin facilitates the TRBP-RNA interaction, and the RNAi-enhancing activity is TRBP-dependent. Nat Biotechnol . 2008 Aug;26(8):933-40.
  • Enoxacin enhances miRNA production through binding to TRBP protein. Proc Natl Acad Sci U S A . 2011 Mar 15;108(11):4394-9.
  • Enoxacin growth-inhibitory and miRNA-enhancing expression is TRBP-dependent. Proc Natl Acad Sci U S A . 2011 Mar 15;108(11):4394-9.
Contact Us Back to top