1. Anti-infection
  2. Bacterial Antibiotic
  3. Orbifloxacin

Orbifloxacin is an orally administrable Antibiotic. Orbifloxacin disrupts the replication and proliferation of Bacterial DNA, inhibits bacterial growth and exerts bactericidal activity. Orbifloxacin inhibits the growth of canine-derived E. coli and Pseudomonas aeruginosa isolates. Orbifloxacin is used in research related to bacterial infections.

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Orbifloxacin

Orbifloxacin Chemische Struktur

CAS. Nr. : 113617-63-3

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Beschreibung

Orbifloxacin is an orally administrable Antibiotic. Orbifloxacin disrupts the replication and proliferation of Bacterial DNA, inhibits bacterial growth and exerts bactericidal activity. Orbifloxacin inhibits the growth of canine-derived E. coli and Pseudomonas aeruginosa isolates. Orbifloxacin is used in research related to bacterial infections[1][2][3][4].

IC50 & Target

Quinolone

 

In Vitro

Orbifloxacin (0.015-4.0 μg/mL; up to 7 days) inhibits the growth of Piscirickettsia salmonis LF-89 VR-1361, and its growth-inhibitory effect persists throughout the 7-day incubation period compared with the untreated control group[1].
Orbifloxacin (0.1×-4× MIC; 0-24 h) inhibits the growth of Staphylococcus aureus ATCC 29213 and ATCC 43300, with MIC values of 0.5 mg/L and 4 mg/L, respectively, and induces concentration-dependent post-antibiotic effect (PAE) and post-antibiotic sub-MIC effect (PA-SME)[2].
Orbifloxacin (at twice the MIC; 1 h) induces a post-antibiotic effect (PAE) with an average duration of 0.29 h in clinical canine isolates of E coli, and an average PAE duration of 0.37 h in clinical canine isolates of Pseudomonas aeruginosa[3].
Orbifloxacin (0.1×MIC-0.3×MIC) induces concentration-dependent PA-SMEs in canine clinical isolates of E coli (mean 0.55 to 2.03 h) and Pseudomonas aeruginosa (mean 1.04 to 2.47 h)[3].
Orbifloxacin (0.016-16 mg/L; 18 h) inhibits visible growth of clinical Staphylococcus intermedius strains isolated from canine skin and ear infections by 50% and 90% at concentrations of 0.5 mg/L and 1 mg/L, respectively[4].
Orbifloxacin (0.063-4 mg/L; 1-24 h) exhibits concentration-dependent bactericidal activity against Staphylococcus aureus ATCC 29213, and time-dependent bactericidal activity against Staphylococcus intermedius isolates from pyoderma[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-last AUC0-∞ Vd/F CL/F MRT0-last F Vd CL
Mice[2] 2.5 mg/kg i.v. 1.09 h 0.08 h 1.96 mg/L 1.72 μg·h/mL 1.74 μg·h/mL / / 1 h / 2.28 L/kg 1.47 L/h/kg
Mice[2] 5 mg/kg i.v. 1.12 h 0.08 h 3.78 mg/L 4.78 μg·h/mL 4.86 μg·h/mL / / 1.29 h / 1.67 L/kg 1.04 L/h/kg
Mice[2] 20 mg/kg i.v. 2.08 h 0.08 h 8.84 mg/L 17.06 μg·h/mL 17.09 μg·h/mL / / 1.84 h / 3.64 L/kg 1.20 L/h/kg
Mice[2] 80 mg/kg i.v. 1.95 h 0.19 h 21.8 mg/L 54.94 μg·h/mL 54.98 μg·h/mL / / 3.17 h / 4.18 L/kg 1.48 L/h/kg
Mice[2] 2.5 mg/kg i.m. 1.36 h 0.25 h 1.45 mg/L 1.73 μg·h/mL 1.77 μg·h/mL 2.96 L/kg 1.47 L/h/kg 1.14 h 99.9 % / /
Mice[2] 5 mg/kg i.m. 1.42 h 0.22 h 4.18 mg/L 5.12 μg·h/mL 5.15 μg·h/mL 2.00 L/kg 0.98 L/h/kg 1.31 h 107.5 % / /
Mice[2] 20 mg/kg i.m. 2.24 h 0.25 h 9.03 mg/L 18.80 μg·h/mL 18.85 μg·h/mL 3.60 L/kg 1.14 L/h/kg 1.94 h 109.2 % / /
Mice[2] 80 mg/kg i.m. 2.02 h 0.25 h 27.13 mg/L 53.94 μg·h/mL 53.98 μg·h/mL 4.43 L/kg 1.52 1.74 h 98.2 % / /
In Vivo

Orbifloxacin (2.5-80 mg/kg; i.m.; twice daily; 24 hours) has an AUC24h/MIC ratio (R2 > 0.98) that is a strong predictor of its in vivo antibacterial efficacy against S. aureus, with targets of 33.78-37.79 h for bacteriostatic activity and 179.43-217.47 h for 3-log10 bacterial kill[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c (specific-pathogen-free, 6 weeks old, both sexes, 18 to 20 g, neutropenic thigh infection model induced via intraperitoneal cyclophosphamide)[2]
Dosage: 2.5 mg/kg ; 5 mg/kg ); 20 mg/kg; 80 mg/kg
Administration: i.m.; twice daily; 24 hours
Result: Partially inhibited bacterial growth over 24 hours at total daily doses of 5 and 10 mg/kg.
Inhibited bacterial replication at a total daily dose of 40 mg/kg.
Reduced the bacterial load in the thigh by a maximum of 3.12 log10 over 24 hours at a maximum total daily dose of 160 mg/kg.
Molekulargewicht

395.38

Formel

C19H20F3N3O3

CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CN(C2CC2)C3=C(C(F)=C(F)C(N4C[C@H](C)N[C@H](C)C4)=C3F)C1=O)O

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 6 mg/mL (15.18 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5292 mL 12.6461 mL 25.2921 mL
5 mM 0.5058 mL 2.5292 mL 5.0584 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molaritätsrechner

  • Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Reinheit & Dokumentation
Verweise

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5292 mL 12.6461 mL 25.2921 mL 63.2303 mL
5 mM 0.5058 mL 2.5292 mL 5.0584 mL 12.6461 mL
10 mM 0.2529 mL 1.2646 mL 2.5292 mL 6.3230 mL
15 mM 0.1686 mL 0.8431 mL 1.6861 mL 4.2154 mL
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  • Do most proteins show cross-species activity?

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