氯唑西林钠一水合物
中文名称:
氯唑西林钠一水合物
中文同义词:
氯唑青霉素钠水合物;邻氯苯甲异唑青;邻氯苯甲异唑青霉素钠;3,3-二甲基-6-[5-甲基-3-(2-氯苯基)-4-异噁唑甲酰氨基]-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚烷-2-甲酸钠盐;氯唑西林钠;邻氯苯甲异恶唑青霉素钠;邻氯苯唑西林钠;氯唑西林钠一水合物
英文名称:
Sodium cloxacillin monohydrate
英文同义词:
bactopen;brl-1621sodiumsaltmonohydrate;cloxacillinsodiummonohydrate;CLOXACILLIN SODIUM SALT MONOHYDRATE;CLOXACILLIN SODIUM SALT HYDRATE;CLOXACILLIN SODIUM SALT N-HYDRATE;CLOXACILLIN SODIUM SALT HYDRATE VETRANAL;CLOXACILLIN SODIUM EPC(CRM STANDARD)
CAS号:
7081-44-9
分子式:
C19H19ClN3NaO6S
分子量:
475.88
EINECS号:
629-588-2
相关类别:
抗生素类;医药原料药;合成;医药原料;小分子抑制剂;医药化工类;分析标准品;抗生素;Principle;Antibiotics;C;Neats;Peptide Synthesis/Antibiotics;抗生素及抗病毒;TEGOPEN;青霉素类;β-内酰胺类抗生素;其他原料药;医用原料;农用兽用原料;科研试剂;原料;兽药原料药;原料药;Antibiotics for Research and Experimental Use;beta-Lactams (Antibiotics for Research and Experimental Use);Biochemistry;1694 PharmaceuticalsPersonal Care Products;BactericidalAntibiotics;beta-Lactam StructureAlphabetic;Chemical Structure;CI - CLEPA;Interferes with Cell Wall SynthesisEPA;A - KAntibiotics;Antibacterial;Antibiotics A to;Antibiotics A-FAntibiotics;Chemical Structure Class;Mechanism of Action;NeatsAntibiotics;Penicillins and Cephalosporins (beta-Lactams);Spectrum of Activity
Mol文件:
7081-44-9.mol
熔点
170℃
沸点
689℃
闪点
>110°(230°F)
储存条件
2-8°C
溶解度
H2O: soluble50mg/mL
形态
solid
水溶解性
Soluble in water
Merck
13,2444
BRN
5403885
CAS 数据库
7081-44-9(CAS DataBase Reference)
生物活性
Cloxacillin Sodium是Cloxacillin的钠盐形式，是一种耐青霉素酶，耐酸，半合成的青霉素。
体外研究
Cloxacillin is an antibiotic useful for the study of a number of bacterial infections.
Cell Viability Assay
Cell Line: Strains M12 and M60.
Concentration: 0.5 μg/mL.
Incubation Time: 4-24 h.
Result: Significantly reduced the bacterial numbers.
Cell Line:
Strains M12 and M60.
Concentration:
0.5 μg/mL.
Incubation Time:
4-24 h.
Result:
Significantly reduced the bacterial numbers.
体内研究
Cloxacillin sodium (50 mg/kg, Subcutaneously) results a significant antibiotic efficacy against S. aureus .
Animal Model: Mice.
Dosage: 10 mg/kg ( Pharmacological Analysis ).
Administration: Given subcutaneously.
Result: Reached a maximal concentration in plasma of 8.4 μg/mL at 10 min and had a half-life of approximately 15 min.
Animal Model: Mice injected with approximately 2 × 10 6 CFU of bacteria in 0.1 mL saline were aseptically injected into the right thigh muscle.
Dosage: 0–500 mg/kg.
Administration: Subcutaneously in the nuchal region at 1 h after infection.
Result: Resulted in a significant decrease in the number of viable S. aureus measured 18 h thereafter.
Animal Model:
Mice.
Dosage:
10 mg/kg ( Pharmacological Analysis ).
Administration:
Given subcutaneously.
Result:
Reached a maximal concentration in plasma of 8.4 μg/mL at 10 min and had a half-life of approximately 15 min.
Animal Model:
Mice injected with approximately 2 × 10 6 CFU of bacteria in 0.1 mL saline were aseptically injected into the right thigh muscle.
Dosage:
0–500 mg/kg.
Administration:
Subcutaneously in the nuchal region at 1 h after infection.
Result:
Resulted in a significant decrease in the number of viable S. aureus measured 18 h thereafter.
化学性质
白色粉末或结晶性粉末。熔点170℃（分解）。易溶于水，溶于乙醇，微溶于氯仿，有引湿性，微臭，味苦。
用途
该品为半合成抗菌素，与苯唑西林的作用特点和用途均极相似，对耐药金葡菌该品有杀菌作用。口服或肌注吸收较好，血浓度比苯唑西林高2倍，主要用于耐药金葡菌所致感染，如败血症、骨髓炎、皮肤软组织感染、心内膜炎、泌尿系统感染及脑膜炎等疗效较好。
生产方法
邻甲苯胺经重氮化、置换、氯化、水解、肟化等操作。得到邻氯苯甲肟氯，然后与乙酰乙酸乙酯环合、用五氯化磷氯化，得到3-邻氯苯基-5-甲基-4异噁酰氯，最后与6-APA缩合得到邻氯青霉素碱、加异辛酸钠成盐、即为邻氯青霉素钠。
危险品标志
Xn
危险类别码
36/37/38-42/43
安全说明
26-36
WGK Germany
2
RTECS号
XH8920000
海关编码
29411099
