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Marbofloxacin

产品号 S1464 公司名称 Selleck Chemicals
CAS号 115550-35-1 公司网站 http://www.selleckchem.com
分子式 C17H19FN4O4 电 话 (877) 796-6397
分子量 362.3555632 传 真 (832) 582-8590
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产品别名

标题
Marbofloxacin
IUPAC标准名
7-fluoro-2-methyl-6-(4-methylpiperazin-1-yl)-10-oxo-4-oxa-1,2-diazatricyclo[7.3.1.0^{5,13}]trideca-5(13),6,8,11-tetraene-11-carboxylic acid
IUPAC传统名
marbofloxacin
别名
Marbocyl
Zeniquin

产品登记号

CAS号 115550-35-1

产品性质

成盐信息 Free Base
保存条件 -20°C

产品详细信息

详细说明 (English)
Research Area
Description Infection
Biological Activity
Description Marbofloxacin is a potent antibiotic inhibiting bacterial DNA replication.
Targets
IC50
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]
Clinical Trials
Features
Protocol
Animal Study [1]
Animal Models SPF piglets inoculated intratracheally with M. hyopneumoniae strain 116
Formulation Dissolved DMSO, and diluted in saline
Doses ~2 mg/kg/day
Administration Intramuscular injection
References
[1] Le Carrou J, et al. Antimicrob Agents Chemother, 2006, 50(6), 1959-1966.
[2] Vouldoukis I, et al. Vet Parasitol, 2006, 135(2), 137-146.
[3] Voermans M, et al. J Vet Pharmacol Ther, 2006, 29(6), 555-560.

参考文献