Marbofloxacin Chemical Structure

Marbofloxacin Chemical Structure
Molecular Weight: 362.36

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Product Description

Biological Activity

Description Marbofloxacin is a potent antibiotic inhibiting bacterial DNA replication.
Targets Topoisomerase II [1] Topoisomerase IV [1]
In vitro Marbofloxacin is a fluoroquinolone antimicrobial agent developed exclusively for veterinary use. Marbofloxacin exhibits high bactericidal activity against a broad spectrum of aerobic Gram-negative and some Gram-positive bacteria, as well as Mycoplasma spp. As the third generation fluoroquinolone, Marbofloxacin also mainly targets replication and transcription enzymes such as DNA gyrase and topoisomerase IV, which are both essential for bacterial viability. Marbofloxacin has a mycoplasmacidal effect during the exponential phase but not during the lag phase, in both the M. hyopneumoniae 116 wild-type strain and a clone isolated 4 days post-marbofloxacin treatment in vivo at the therapeutic dose. [1] Marbofloxacin significantly kills Leishmania promastigotes and intracellular amastigotes in a dose-dependent manner, more efficient than meglumine antimoniate and sodium stibogluconate. After treatment with Marbofloxacin, macrophages acquire resistance to infection and enhanced antileishmanial activity through the NO synthase pathway. [2]
In vivo Marbofloxacin treatment at the therapeutic dose does not eliminate M. hyopneumoniae, with 87.5 to 100% of the pigs still positive at the end of the assays, and is not effective in significantly reducing clinical signs. Nevertheless, Marbofloxacin treatment seems to decrease the lung lesion scores. [1] Administration of Marbofloxacin at 6 mg/kg once daily for 7 days in a Staphylococcus aureus infection in tissue cages in ponies is not effective for the elimination of S. aureus infections from secluded sites. [3]
Features

Protocol(Only for Reference)

Animal Study: [1]

Animal Models SPF piglets inoculated intratracheally with M. hyopneumoniae strain 116
Formulation Dissolved DMSO, and diluted in saline
Dosages ~2 mg/kg/day
Administration Intramuscular injection

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[2] Vouldoukis I, et al. Vet Parasitol, 2006, 135(2), 137-146.

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Chemical Information

Download Marbofloxacin SDF
Molecular Weight (MW) 362.36
Formula

C17H19FN4O4

CAS No. 115550-35-1
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 3 mg/mL warming (8.27 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80, pH 4 14 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-3,7-dihydro-2H-[1,3,4]oxadiazino[6,5,4-ij]quinoline-6-carboxylic acid

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