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相关CAS号：
51762-05-1 38821-53-3
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51762-05-1

51762-05-1结构式
51762-05-1结构式
  • 常用中文名：头孢沙定
  • 常用英文名：Cefroxadine
  • CAS号：51762-05-1
  • 分子式：C16H19N3O5S
  • 分子量：365.40400
  • 相关类别： 原料药 抗生素类药物 头孢菌素类药
  • 发布时间：2018-08-04 14:55:48
  • 更新时间：2024-01-11 16:39:27
  • 头孢烷(CGP 9000)是一种口服活性头孢菌素抗生素。头孢哌啶对大肠杆菌和肺炎克雷伯菌的MIC值分别为3.13和1.56μg/mL,浓度为106μg/mL。头孢哌啶可用于感染研究[1]。

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中文名 头孢沙定
英文名 Cefroxadine
中文别名 头孢环烯氨
(6R,7R)-7-[[(2R)-2-氨基-2-(1-环己-1,4-二烯)乙酰]氨基]-3-甲氧基-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-甲酸
英文别名 cgp9000
(6R)-7t-((R)-2-amino-2-cyclohexa-1,4-dienyl-acetylamino)-3-methoxy-8-oxo-(6rH)-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Oraspor
antibioticcgp9000
cxd
7-(d-2-amino-2-(1,4-cyclohexadienyl)acetamide)-3-methoxy-3-cephem-4-carboxyl
cefroxadin
7-[2-aMino-2-(cyclohexa-2,5-dien-1-yl)acetaMido]-3-Methoxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
描述 头孢烷(CGP 9000)是一种口服活性头孢菌素抗生素。头孢哌啶对大肠杆菌和肺炎克雷伯菌的MIC值分别为3.13和1.56μg/mL,浓度为106μg/mL。头孢哌啶可用于感染研究[1]。
相关类别
体外研究 头孢哌啶(106-108μg/mL；过夜)对金黄色葡萄球菌、大肠杆菌、伤寒链球菌、副伤寒链霉菌、肖特穆埃利链球菌、呼吸暂停链球菌和奇异链球菌具有抗菌活性,其MIC值分别为1.56、3.31、1.56、1.56,1.56、15.6和6.25μg/mL,浓度为106μg/mL[1]。头孢哌啶(104-108μg/mL；过夜)对100株大肠杆菌菌株显示出抗菌活性,MIC50和MIC75值分别为4.8-11.5μg/mL和6-20μg/mL[1]。
体内研究 头孢哌啶(0-30 mg/kg；感染后0和3小时口服)在体内表现出比头孢氨苄更好的效果[1]。动物模型：感染大肠杆菌ML4707和肺炎克雷伯菌GN6445的小鼠[1]剂量：0-30 mg/kg给药：口服灌胃；0-30毫克/千克；结果：在体内对大肠杆菌ML4707和肺炎克雷伯菌GN6445的ED50值分别为21.4和10.9 mg/kg,显示出比头孢氨苄更好的效果。
密度 1.5 g/cm3
沸点 719.3ºC at 760 mmHg
熔点 170° (dec)
分子式 C16H19N3O5S
分子量 365.40400
闪点 388.8ºC
精确质量 365.10500
PSA 147.26000
LogP 0.96170
折射率 1.678
储存条件 库房低温通风干燥

CHEMICAL IDENTIFICATION

RTECS NUMBER :
XI0335000
CHEMICAL NAME :
5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-((amino-1,4-cyclohexadien-1- ylacetyl)amino)-3-methoxy-8-oxo-, (6R-(6-alpha,7-beta(R*)))-
CAS REGISTRY NUMBER :
51762-05-1
LAST UPDATED :
199806
DATA ITEMS CITED :
17
MOLECULAR FORMULA :
C16-H19-N3-O5-S
MOLECULAR WEIGHT :
365.44
WISWESSER LINE NOTATION :
T46 ANV ES GUTJ GO1 HVQ CMV1- AL6U DUTJ BZ

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 :
>22500 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 28(Suppl 3),98,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
6 gm/kg
TOXIC EFFECTS :
Behavioral - ataxia Gastrointestinal - hypermotility, diarrhea Skin and Appendages - hair
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 28(Suppl 3),98,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>15 gm/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - altered sleep time (including change in righting reflex) Skin and Appendages - hair
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 28(Suppl 3),98,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>13500 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 28(Suppl 3),98,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
7090 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 29,653,1976
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
13500 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 28(Suppl 3),98,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>1 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,689,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
10 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,APP-11,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
>4 gm/kg
TOXIC EFFECTS :
Kidney, Ureter, Bladder - structural or functional changes in ureter Kidney, Ureter, Bladder - other changes
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 28(Suppl 3),98,1980 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
56 gm/kg/28D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - urine volume increased Kidney, Ureter, Bladder - changes in bladder weight Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 28(Suppl 3),131,1980
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
182 gm/kg/13W-C
TOXIC EFFECTS :
Kidney, Ureter, Bladder - other changes in urine composition Blood - normocytic anemia Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 28(Suppl 3),103,1980
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
27800 mg/kg/26W-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - urine volume increased Endocrine - changes in adrenal weight Endocrine - changes in spleen weight
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 28(Suppl 3),116,1980
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
455 gm/kg/13W-C
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in bladder weight Endocrine - changes in adrenal weight Related to Chronic Data - death
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 28(Suppl 3),103,1980
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
2500 mg/kg/5D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - urine volume increased Kidney, Ureter, Bladder - changes in bladder weight
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 28(Suppl 3),131,1980 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
27 gm/kg
SEX/DURATION :
female 17-22 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - urogenital system
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,615,1980
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
27 gm/kg
SEX/DURATION :
female 17-22 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - live birth index (measured after birth)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,615,1980
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
2700 mg/kg
SEX/DURATION :
female 17-22 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4) Reproductive - Effects on Newborn - delayed effects
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,615,1980


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