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头孢克洛

头孢克洛用途

Cefaclor monohydrate 是一种有效的抗生素,可特异性地结合青霉素结合蛋白 (PBP 3)。

头孢克洛名称

[ CAS 号 ]:
70356-03-5

[ 中文名 ]:
头孢克洛

[ 英文名 ]:
Cefaclor Monohydrate

[中文别名 ]:

[英文别名 ]:

MFCD00071999
Cefaclor monohydrate
EINECS 258-909-5

头孢克洛生物活性

[ 描述 ]:

Cefaclor monohydrate 是一种有效的抗生素,可特异性地结合青霉素结合蛋白 (PBP 3)。

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[参考文献]

[1]. Chambers HF, et al. Characterization of penicillin-binding protein 2 of Staphylococcus aureus: deacylation reaction and identification of two penicillin-binding peptides. Antimicrob Agents Chemother. 1992 Mar;36(3):656-61.

头孢克洛物理化学性质

[ 沸点 ]:
713.4ºC at 760 mmHg

[ 熔点 ]:
>180ºC (dec.)

[ 分子式 ]:
C₁₅H₁₆ClN₃O₅S

[ 分子量 ]:
385.82300

[ 闪点 ]:
385.2ºC

[ 精确质量 ]:
385.05000

[ PSA ]:
147.26000

[ LogP ]:
1.58610

[ 外观性状 ]:
白色晶体粉末

[ 储存条件 ]:
库房低温通风干燥

头孢克洛毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XI0365000

CHEMICAL NAME :: 5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-((aminophenylacetyl)amino)-3- chloro-8-oxo-, monohydrate, (6R-(6-alpha,7-beta(R*)))-

CAS REGISTRY NUMBER :: 70356-03-5

LAST UPDATED :: 199706

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C15-H14-Cl-N3-O4-S.H2-O

MOLECULAR WEIGHT :: 385.85

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >20 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 13,637,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1259 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 13,637,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 4838 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 13,637,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >20 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 13,637,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1227 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 13,637,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4180 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 13,637,1982

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting

REFERENCE :: PMESAJ Postgraduate Medical Journal, Supplement. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.1- 1949- Volume(issue)/page/year: 55(Suppl 4),17,1979

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea

REFERENCE :: PMESAJ Postgraduate Medical Journal, Supplement. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.1- 1949- Volume(issue)/page/year: 55(Suppl 4),17,1979

头孢克洛安全信息

[ 符号 ]:

GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H317-H334

[ 警示性声明 ]:
P261-P280-P284-P304 + P340-P333 + P313-P342 + P311

[ 危害码 (欧洲) ]:
Xn,Xi

[ 风险声明 (欧洲) ]:
42/43-36

[ 安全声明 (欧洲) ]:
22-36/37-45

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
SJ6069000

[ 海关编码 ]:
3004201500

头孢克洛制备

以青霉素G为原料。先用对硝基苄基把青霉素G上的羧基保护起来，然后用双氧水或过氧乙酸氧化成亚砜。在N-氯代丁二酰亚胺或N-氯代磷苯二甲酰胺等作用下，进行氯化和扩环。先臭氧化后还原，使3位形成羟基。然后先在三氯化磷下，使3位转化为氯代；再在五氯化磷和吡啶作用下，接着醇解7位形成游离的氨基的盐酸盐，即7-氨基-3-氯-3-头孢烯-4-羧酸对硝基苄酯的盐酸盐。其溶于四氢呋喃和甲醇的溶液中，加入5%钯-炭的乙醇溶液，在室温和0.35MPa的氢压下氢化反应45min。过滤，滤饼用四氢呋喃和水洗。蒸发溶剂至干。剩余物溶入水和乙酸乙酯的混合液中，Ph值调至3，析出固体，过滤，并用丙酮浸泡，然后干燥即为7-氨基-3-氯-3-头孢烯-4-羧酸。将其溶入乙腈中，在室温搅拌下加入N，O-双(三甲基硅)乙酰胺，使形成可溶性的双硅酯。冷至0℃，在二滴N，N-二甲基苄胺存在下，缓慢加入3-(β-羧基苄胺)丁烯酸甲酯的钠盐和氯甲酸甲酯在乙腈的反应液中。该混合液继续在冰浴中搅拌2h，加入甲醇，过滤除去不溶物。再加入水，调Ph值至1.5，再用三乙胺调至4.5。在水浴上再搅拌1h，过滤析出的结晶性沉淀，用乙腈洗，真空干燥得头孢克洛。

前面得到的游离氨基的盐酸盐，可以先直接和叠氮苯乙酸反应，然后氢解也可得到头孢克罗，其反应较简单。

头孢克洛海关

[ 海关编码 ]: 3004201500

头孢克洛文献

Determination of cefaclor by UPLC-MS-MS for a Chinese pharmacokinetic study.

J. Chromatogr. Sci. 52(7) , 636-40, (2014)

A novel method has been developed for the determination of cefaclor in human plasma by ultra-performance liquid chromatography combined with tandem mass spectrometry (UPLC-MS-MS). The plasma was treat...

A method for rapid screening of interactions of pharmacologically active compounds with albumin.

Anal. Chim. Acta 855 , 51-9, (2014)

We determine the association constants for ligand-protein complex formation using the flow injection method. We carry out the measurements at high flow rates (F=1 mL min(-1)) of a carrier phase. There...

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