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KB-5246
- names：
KB-5246
- CAS号：
119474-55-4
MDL Number： MFCD00877050 - MF(分子式)： C18H17ClFN3O4S MW(分子量)： 425.86
- EINECS: Reaxys Number:
- Pubchem ID:163306678 Brand:BIOFOUNT
KB-5246(119474-55-4,CTK0H7912)是一种四环喹诺酮，KB-5246具有抗菌活性。
| 货品编码 | 规格 | 纯度 | 价格 (¥) | 现价(¥) | 特价(¥) | 库存描述 | 数量 | 总计 (¥) |
|---|---|---|---|---|---|---|---|---|
| YZM000412-1mg | 1mg | >97% | ¥ 14644.50 | ¥ 14644.50 | 2-3天 | ¥ 0.00 |
| 中文别名 | KB-5246(119474-55-4);3H，8H-4-Oxa-1-thia-9b-氮杂环戊基[cd]苯-9-9-羧酸，6-氟-5-（4-甲基-1-哌嗪基）-8-氧代-，盐酸盐(1:1);CTK0H7912; |
| 英文别名 | KB-5246(119474-55-4);3H,8H-4-Oxa-1-thia-9b-azacyclopenta[cd]phenalene-9-carboxylicacid, 6-fluoro-5-(4-methyl-1-piperazinyl)-8-oxo-, hydrochloride (1:1);CTK0H7912; |
| CAS号 | 119474-55-4 |
| SMILES | [H]Cl.CN1CCN(C2=C(F)C=C3C4=C2OCC5=CSC(N45)=C(C(O)=O)C3=O)CC1 |
| Inchi | InChI=1S/C18H18FN3O4S.ClH/c1-21-2-4-22(5-3-21)15-14(19)8-6-10(23)13(18(24)25)17-11(8)12-9(20-27-17)7-26-16(12)15;/h11-12H,2-7H2,1H3,(H,24,25);1H |
| InchiKey | URZNPRNEDQSWGC-UHFFFAOYSA-N |
| 分子式 Formula | C18H17ClFN3O4S |
| 分子量 Molecular Weight | 425.86 |
| 闪点 FP | |
| 熔点 Melting point | 287 °C (decomp) |
| 沸点 Boiling point | |
| Polarizability极化度 | |
| 密度 Density | |
| 蒸汽压 Vapor Pressure | |
| 溶解度Solubility | |
| 性状 | Solid |
| 储藏条件 Storage conditions | 室温,请根据产品建议的存储条件进行存储,Please store the product under the recommended condition sin the description. |
KB-5246(119474-55-4,CTK0H7912)毒理性质：
| 生物 | 测试类型 | 路线 | 报告剂量（标准化剂量） | 影响 | 资源 |
| mouse | LD50 | intravenous | 237mg/kg (237mg/kg) | Journal of Medicinal Chemistry. Vol. 35, Pg. 94, 1992. | |
| mouse | LD50 | oral | 1231mg/kg (1231mg/kg) | Journal of Medicinal Chemistry. Vol. 35, Pg. 94, 1992. |
KB-5246(119474-55-4,CTK0H7912)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.
Tags:KB-5246试剂,KB-5246合成,KB-5246中间体,KB-5246杂质,KB-5246密度,KB-5246溶解度,KB-5246旋光度,KB-5246闪点,KB-5246熔点,KB-5246购买,
| 产品说明 | KB-5246(119474-55-4,CTK0H7912)是一种四环喹诺酮，KB-5246具有抗菌活性。 |
| Introduction | KB-5246(119474-55-4,CTK0H7912)is a tetracyclic quinolone and displays antibacterial activities. |
| Application1 | |
| Application2 | |
| Application3 |
KB-5246(119474-55-4,CTK0H7912)药理学：
1、KB-5246是四环喹诺酮，具有抗菌活性。90％的KB-5246分离株（MIC90s）对革兰氏阳性菌如金黄色葡萄球菌（包括耐甲氧西林的金黄色葡萄球菌，表皮葡萄球菌，肺炎链球菌和化脓链球菌）的MIC为0.39μg / mL。KB5246抑制90％的分离株的大肠杆菌，肺炎克雷伯氏菌，产酸克雷伯菌在0.10微克/ mL的浓度或更少。当添加MIC或更高浓度的KB-5246时，孵育24小时后未观察到再生长。
2、KB-5246对肺炎链球菌 2132感染的50％有效剂量值为50.5 mg / kg体重。KB-5246对金黄色葡萄球菌史密斯，铜绿假单胞菌 GN11189和粘质沙雷氏菌 GN7577感染的活性与氧氟沙星相当，但大于诺氟沙星。
| 警示图 | |
| 危险性 | warning |
| 危险性警示 | Not available |
| 安全声明 | H303吞入可能有害+H313皮肤接触可能有害+H2413吸入可能对身体有害 |
| 安全防护 | P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P2393获得医疗建议/护理 |
| 备注 | 实验过程中防止吸入、食入，做好安全防护 |
| Kotera Y, et al. In vitro and in vivo antibacterial activities of KB-5246, a new tetracyclic quinolone. Antimicrob Agents Chemother. 1989 Nov;33(11):1896-900. |
KB-5246(119474-55-4,CTK0H7912)参考文献：
1、In vitro and in vivo antibacterial activities of KB-5246, a new tetracyclic quinolone
Y Kotera 1, S Mitsuhashi
Abstract The in vitro and in vivo antibacterial activities of KB-5246, a tetracyclic quinolone, were compared with those of ciprofloxacin, ofloxacin, and norfloxacin. KB-5246 demonstrated a broad antibacterial spectrum. The in vitro activity of KB-5246 against gram-negative bacteria was higher than that of ofloxacin or norfloxacin and was comparable to that of ciprofloxacin. KB-5246 demonstrated the greatest activity against gram-positive bacteria of the four agents tested. Among Streptococcus pyogenes strains resistant to 1.56 micrograms of norfloxacin per ml, there were 26 strains susceptible to 0.2 micrograms of KB-5246 per ml. Similarly, among the Staphylococcus aureus and Staphylococcus epidermidis strains resistant to 3.13 micrograms of norfloxacin per ml, there were 23 S. aureus and 11 S. epidermidis strains susceptible to 0.39 micrograms of KB-5246 per ml. Among the Streptococcus pneumoniae and Enterococcus faecalis strains resistant to 12.5 micrograms of norfloxacin per ml, there were 5 S. pneumoniae and 10 E. faecalis strains susceptible to 0.39 micrograms of KB-5246 per ml. KB-5246 had bactericidal activity at the MIC. KB-5246 demonstrated excellent antibacterial activity against various systemic infections in mice. After oral administration, KB-5246 was as active as ofloxacin and about two times more active than norfloxacin.
1、In vitro and in vivo antibacterial activities of KB-5246, a new tetracyclic quinolone
Y Kotera 1, S Mitsuhashi
Abstract The in vitro and in vivo antibacterial activities of KB-5246, a tetracyclic quinolone, were compared with those of ciprofloxacin, ofloxacin, and norfloxacin. KB-5246 demonstrated a broad antibacterial spectrum. The in vitro activity of KB-5246 against gram-negative bacteria was higher than that of ofloxacin or norfloxacin and was comparable to that of ciprofloxacin. KB-5246 demonstrated the greatest activity against gram-positive bacteria of the four agents tested. Among Streptococcus pyogenes strains resistant to 1.56 micrograms of norfloxacin per ml, there were 26 strains susceptible to 0.2 micrograms of KB-5246 per ml. Similarly, among the Staphylococcus aureus and Staphylococcus epidermidis strains resistant to 3.13 micrograms of norfloxacin per ml, there were 23 S. aureus and 11 S. epidermidis strains susceptible to 0.39 micrograms of KB-5246 per ml. Among the Streptococcus pneumoniae and Enterococcus faecalis strains resistant to 12.5 micrograms of norfloxacin per ml, there were 5 S. pneumoniae and 10 E. faecalis strains susceptible to 0.39 micrograms of KB-5246 per ml. KB-5246 had bactericidal activity at the MIC. KB-5246 demonstrated excellent antibacterial activity against various systemic infections in mice. After oral administration, KB-5246 was as active as ofloxacin and about two times more active than norfloxacin.
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