| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
The primary target of (R)-Ofloxacin is bacterial DNA gyrase and topoisomerase IV, similar to other fluoroquinolones. However, the R-enantiomer has significantly reduced activity compared to the S-enantiomer. It binds to the enzymes but with lower affinity, resulting in weaker inhibition of DNA replication and bacterial cell death. The compound's reduced activity makes it useful for studying stereoselectivity.
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| ln Vitro |
In vitro, (R)-Ofloxacin has significantly reduced antibacterial activity compared to levofloxacin. It is used as a negative control or as a tool to study the stereoselectivity of fluoroquinolone antibiotics. The compound's reduced activity has been confirmed in various in vitro susceptibility tests.
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| ln Vivo |
In vivo, (R)-Ofloxacin is not used as a therapeutic agent due to its reduced antibacterial activity. It is used in research to study the pharmacokinetics and pharmacodynamics of ofloxacin enantiomers. The compound is primarily used as an analytical standard and in research applications.
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| Enzyme Assay |
In vitro enzyme or receptor binding assays for (R)-Ofloxacin involve measuring its inhibition of DNA gyrase and topoisomerase IV activity. The assay uses purified recombinant enzymes and a DNA substrate. The supercoiling or relaxation of DNA is measured using gel electrophoresis or a fluorescent method. The compound is incubated with the enzyme and substrate at varying concentrations, and the IC50 is determined and compared to that of levofloxacin.
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| Cell Assay |
In vitro cell-based assays for (R)-Ofloxacin are performed using bacterial cultures to determine the minimum inhibitory concentration (MIC). The compound's antibacterial activity is compared to that of levofloxacin. The MIC for (R)-Ofloxacin is significantly higher than for levofloxacin, reflecting its reduced activity.
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| Animal Protocol |
In vivo animal experiments for (R)-Ofloxacin are limited, as it is not a therapeutic agent. It may be used in pharmacokinetic studies to compare the distribution and elimination of ofloxacin enantiomers. The compound is administered orally or intravenously, and plasma concentrations are measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of (R)-Ofloxacin are similar to those of levofloxacin. The compound has a molecular weight of 361.37 and a molecular formula of C18H20FN3O4. It is a solid at room temperature. The compound is well-absorbed after oral administration and is widely distributed in tissues. It is metabolized in the liver and excreted renally.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for (R)-Ofloxacin are similar to those of other fluoroquinolones. Common side effects include gastrointestinal disturbances, central nervous system effects, and phototoxicity. The compound should be used with caution in patients with a history of tendon disorders or epilepsy.
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| References | |
| Additional Infomation |
Dextrofloxacin is the (R)-enantiomer of ofloxacin. It is an antibacterial drug and also an EC 5.99.1.3 [DNA topoisomerase (ATP hydrolysis)] inhibitor, topoisomerase IV inhibitor, and DNA synthesis inhibitor. Its chemical name is 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid, belonging to the quinolone and fluoroquinolone antibiotics. It is the enantiomer of levofloxacin.
A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, thereby preventing DNA replication. See also: Levofloxacin (note moved to). Other information: (R)-Ofloxacin is the R-enantiomer of ofloxacin. It is also known as Dextrofloxacin. The S-enantiomer (levofloxacin) is the more active antibacterial agent. The compound is used in research to study stereoselectivity and as an analytical standard. Its CAS number is 100986-86-5. |
| Molecular Formula |
C18H20N3O4F
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|---|---|
| Molecular Weight |
361.3675
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| Exact Mass |
361.143
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| Elemental Analysis |
C, 59.83; H, 5.58; F, 5.26; N, 11.63; O, 17.71
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| CAS # |
100986-86-5
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| Related CAS # |
Ofloxacin;82419-36-1;Levofloxacin;100986-85-4;Levofloxacin hydrate;138199-71-0;Levofloxacin hydrochloride;177325-13-2;Levofloxacin sodium;872606-49-0;(R)-Ofloxacin-d3;1346617-10-4
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| PubChem CID |
452723
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| Appearance |
Solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
571.5±50.0 °C at 760 mmHg
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| Flash Point |
299.4±30.1 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.670
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| LogP |
0.84
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
26
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| Complexity |
634
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| Defined Atom Stereocenter Count |
1
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| SMILES |
FC1=CC2=C3N(C=C(C(O)=O)C2=O)C(C)COC3=C1N1CCN(C)CC1
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| InChi Key |
GSDSWSVVBLHKDQ-SNVBAGLBSA-N
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| InChi Code |
InChI=1S/C18H20FN3O4/c1-10-9-26-17-14-11(16(23)12(18(24)25)8-22(10)14)7-13(19)15(17)21-5-3-20(2)4-6-21/h7-8,10H,3-6,9H2,1-2H3,(H,24,25)/t10-/m1/s1
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| Chemical Name |
(2R)-7-fluoro-2-methyl-6-(4-methylpiperazin-1-yl)-10-oxo-4-oxa-1-azatricyclo[7.3.1.05,13]trideca-5(13),6,8,11-tetraene-11-carboxylic acid
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| Synonyms |
(R)-Ofloxacin, (+)-Ofloxacin; (R)-(+)-Ofloxacin; D-Ofloxacin; DR 3354; DR-3354; DR3354; d-Levofloxacin; Dextrofloxacin;
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| 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) |
DMSO : ~10 mg/mL (~27.67 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 | 2.7672 mL | 13.8362 mL | 27.6725 mL | |
| 5 mM | 0.5534 mL | 2.7672 mL | 5.5345 mL | |
| 10 mM | 0.2767 mL | 1.3836 mL | 2.7672 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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