| 规格 | 价格 | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| 靶点 |
Topoisomerase IV/II
|
|---|---|
| 体外研究 (In Vitro) |
体外活性：马波沙星是一种专为兽医用途开发的氟喹诺酮抗菌剂。 Marbofloxacin 对多种需氧革兰氏阴性菌和一些革兰氏阳性菌以及支原体表现出高杀菌活性。作为第三代氟喹诺酮类药物，马波沙星还主要靶向复制和转录酶，例如 DNA 旋转酶和拓扑异构酶 IV，这两种酶对于细菌的活力都至关重要。在猪肺炎支原体 116 野生型菌株和马波沙星以治疗剂量体内治疗 4 天后分离的克隆中，马波沙星在指数期具有支原体作用，但在滞后期不具有支原体作用。马波沙星以剂量依赖性方式显着杀死利什曼原虫前鞭毛体和细胞内无鞭毛体，比葡甲胺锑酸盐和葡萄糖酸钠更有效。用 Marbofloxacin 治疗后，巨噬细胞获得了对感染的抵抗力，并通过 NO 合酶途径增强了抗利什曼尼活性。[2]
|
| 体内研究 (In Vivo) |
研究发现，马波沙星 6 mg/kg，每日一次，持续 7 天，对于小马组织笼中隐蔽区域的金黄色葡萄球菌感染治疗无效 [2]。在六匹马中静脉内、皮下和口服单剂量 2 mg/kg bwt 后，研究了马波沙星的药代动力学特性，并评估了对从马传染病中分离出的细菌的最小抑制作用。细菌浓度 (MIC)。马波沙星的终末半衰期为 756 +/- 1.99 小时，清除率为平均值 +/- 标准偏差 0.25 +/- 0.05 l/kg/h。皮下和口服给药后，马波沙星的绝对生物利用度分别为 98 +/- 11% 和 62 +/- 8%。考虑到氟喹诺酮疗效指数的断点值，马波沙星静脉、皮下或口服给药方案2 mg/kg体重/24小时对肠杆菌科细菌比对金黄色葡萄球菌更有利[3]。
治疗剂量的马波沙星治疗不能消除猪肺炎支原体，87.5%至100%的猪在检测结束时仍呈阳性，并且不能有效显着减少临床症状。尽管如此，马波沙星治疗似乎降低了肺部病变评分。在小马组织笼内的金黄色葡萄球菌感染中，每天一次给予马波沙星 6 mg/kg，持续 7 天，对于消除隐蔽场所的金黄色葡萄球菌感染无效。[3] |
| 动物实验 |
SPF piglets inoculated intratracheally with M. hyopneumoniae strain 116
~2 mg/kg/day Intramuscular injection Tissue cages (TC), implanted subcutaneously in the neck in eight ponies, were inoculated with Staphylococcus aureus (S. aureus) to determine the clinical efficacy of marbofloxacin in the treatment of this infection. From 21 h after inoculation, marbofloxacin (6 mg/kg) was administered intravenously (i.v.) once daily for 7 days. Samples of the tissue cage fluid (TCF) were taken to determine marbofloxacin concentrations (days 1, 3 and 7), using high-pressure liquid chromatography, and numbers of viable bacteria [colony forming units (CFU)] (days 1, 3, 7, 14 and 21). Statistical analysis was used to compare CFU before and after treatment. Clinical signs and CFU were used to evaluate the efficacy of treatment. Although, there was a slight decrease in CFU in all TC initially, the infection was not eliminated by marbofloxacin treatment in any of the ponies and abscesses formed. As the MIC (0.25 microg/mL) did not change during treatment and the concentration of marbofloxacin during treatment (mean concentration in TCF was 0.89 microg/mL on day 1, 0.80 microg/mL on day 3 and 2.77 microg/mL on day 7) was above MIC, we consider that the treatment failure might be attributable to the formation of a biofilm by S. aureus. Based on the present results, i.v. administration of marbofloxacin alone is not suitable for the elimination of S. aureus infections from secluded sites.[2] |
| 药代性质 (ADME/PK) |
Marbofloxacin is a fluoroquinolone antibiotic expected to be effective in the treatment of infections involving gram-negative and some gram-positive bacteria in horses. In order to design a rational dosage regimen for the substance in horses, the pharmacokinetic properties of marbofloxacin were investigated in 6 horses after i.v., subcutaneous and oral administration of a single dose of 2 mg/kg bwt and the minimal inhibitory concentrations (MIC) assessed for bacteria isolated from equine infectious pathologies. The clearance of marbofloxacin was mean +/- s.d. 0.25 +/- 0.05 l/kg/h and the terminal half-life 756 +/- 1.99 h. The marbofloxacin absolute bioavailabilities after subcutaneous and oral administration were 98 +/- 11% and 62 +/- 8%, respectively. The MIC required to inhibit 90% of isolates (MIC90) was 0.027 microg/ml for enterobacteriaceae and 0.21 microg/ml for Staphylococcus aureus. The values of surrogate markers of antimicrobial efficacy (AUIC, Cmax/MIC ratio, time above MIC90) were calculated and the marbofloxacin concentration profiles simulated for repeated administrations. These data were used to determine rational dosage regimens for target bacteria. Considering the breakpoint values of efficacy indices for fluoroquinolones, a marbofloxacin dosage regimen of 2 mg/kg bwt/24 h by i.v., subcutaneous or oral routes was more appropriate for enterobacteriaceae than for S. aureus. [3]
|
| 毒性/毒理 (Toxicokinetics/TK) |
mouse LD50 oral >2 gm/kg United States Patent Document., #4801584
|
| 参考文献 | |
| 其他信息 |
LSM-5799 is a member of quinolines.
Marbofloxacin is a carboxylic acid, part of the third generation of antibiotic fluoroquinolones. It is used in veterinary medicine. A formulation of marbofloxacin combined with clotrimazole and dexamethasone is available under the name Aurizon. IN THE TITLE COMPOUND, [SYSTEMATIC NAME: 9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-piperazin-1-yl)-7-oxo-7H-pyrido[1,2,3-ij][1,2,4]benzoxadiazine-6-carb-oxy-lic acid], C(17)H(19)FN(4)O(4), the carbonyl and carboxyl groups are coplanar with the quinoline ring, making a dihedral angle of 2.39 (2)°. The piperazine ring adopts a chair conformation and the oxadiazinane ring displays an envelope conformation with the CH(2) group at the flap displaced by 0.650 (2) Å from the plane through the other five atoms. The mol-ecular structure exhibits an S(6) ring motif, owing to an intra-molecular O-H⋯O hydrogen bond. In the crystal, weak C-H⋯F hydrogen bonds link mol-ecules into layers parallel to the ab plane.[1] |
| 分子式 |
C17H20CLFN4O4
|
|---|---|
| 分子量 |
398.8165
|
| 精确质量 |
398.116
|
| CAS号 |
115551-26-3
|
| 相关CAS号 |
Marbofloxacin;115550-35-1
|
| PubChem CID |
14576609
|
| 外观&性状 |
Typically exists as solid at room temperature
|
| LogP |
1.378
|
| tPSA |
78.25
|
| 氢键供体(HBD)数目 |
2
|
| 氢键受体(HBA)数目 |
9
|
| 可旋转键数目(RBC) |
2
|
| 重原子数目 |
27
|
| 分子复杂度/Complexity |
636
|
| 定义原子立体中心数目 |
0
|
| SMILES |
Cl[H].FC1C([H])=C2C(C(C(=O)O[H])=C([H])N3C2=C(C=1N1C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C1([H])[H])OC([H])([H])N3C([H])([H])[H])=O
|
| InChi Key |
OCRYFLKYXNBUEY-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H19FN4O4.ClH/c1-19-3-5-21(6-4-19)14-12(18)7-10-13-16(14)26-9-20(2)22(13)8-11(15(10)23)17(24)25;/h7-8H,3-6,9H2,1-2H3,(H,24,25);1H
|
| 化学名 |
7-fluoro-2-methyl-6-(4-methylpiperazin-1-yl)-10-oxo-4-oxa-1,2-diazatricyclo[7.3.1.05,13]trideca-5(13),6,8,11-tetraene-11-carboxylic acid;hydrochloride
|
| 别名 |
Marbofloxacin (hydrochloride); Marbofloxacin hydrochloride; 115551-26-3; 7-fluoro-2-methyl-6-(4-methylpiperazin-1-yl)-10-oxo-4-oxa-1,2-diazatricyclo[7.3.1.05,13]trideca-5(13),6,8,11-tetraene-11-carboxylic acid;hydrochloride; 9-Fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,3,4]oxadiazino[6,5,4-ij]quinoline-6-carboxylic acid hydrochloride; Marbofloxacinhydrochloride; W3C3ZZ8R2D; SCHEMBL10563057;
|
| HS Tariff Code |
2934.99.9001
|
| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| 溶解度 (体外实验) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 溶解度 (体内实验) |
注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。
注射用配方
注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)(IP/IV/IM/SC等) *生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。 注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline) 注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil) 示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。 View More
注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)] 口服配方
口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠) 口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素) 示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。 View More
口服配方 3: 溶解于 PEG400 (聚乙二醇400) 请根据您的实验动物和给药方式选择适当的溶解配方/方案： 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5074 mL | 12.5370 mL | 25.0740 mL | |
| 5 mM | 0.5015 mL | 2.5074 mL | 5.0148 mL | |
| 10 mM | 0.2507 mL | 1.2537 mL | 2.5074 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
计算结果:
工作液浓度： mg/mL；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
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