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Marbofloxacin 115550-35-1

Product Description

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Marbofloxacin

Molecular Weight: 362.36 Marbofloxacin is a potent antibiotic inhibiting bacterial DNA replication.


Biological Activity


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. 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.


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. 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.


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
Solubility 1% DMSO/30% polyethylene glycol/1% Tween 80, pH 4, 14 mg/mL
* 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.


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


Species Baboon Dog Monkey Rabbit Guinea pig Rat Hamster Mouse
Weight (kg) 12 10 3 1.8 0.4 0.15 0.08 0.02
Body Surface Area (m2) 0.6 0.5 0.24 0.15 0.05 0.025 0.02 0.007
Km factor 20 20 12 12 8 6 5 3

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)




Chemical Information




Molecular Weight (MW) 362.36
Formula

C17H19FN4O4

CAS No. 115550-35-1

Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms



Solubility (25°C) * In vitro DMSO 2 mg/mL (5.51 mM)
Water <1 mg/mL (
Ethanol <1 mg/mL (
In vivo 1% DMSO/30% polyethylene glycol/1% Tween 80, pH 4 14 mg/mL




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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