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3577-01-3

3577-01-3结构式
3577-01-3结构式
  • 常用中文名:头孢来星
  • 常用英文名:Cefaloglycin
  • CAS号:3577-01-3
  • 分子式:C18H19N3O6S
  • 分子量:405.42500
  • 相关类别: 原料药 抗生素类药物 头孢菌素类药
  • 发布时间:2018-08-17 10:31:31
  • 更新时间:2024-01-06 04:19:10
  • Cefaloglycin (Cephaloglycin) 是一种具有口服活性的肾毒性 β-内酰胺类 (β-lactam) 头孢菌素抗生素,具有抗菌活性。Cefaloglycin 对肠球菌以外的革兰氏阳性球菌 (Gram-Positive cocci) 有活性。Cefaloglycin 对线粒体底物的摄取和呼吸也具有毒性。

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中文名 头孢来星
英文名 cefaloglycin
英文别名 Cefaloglycin
Cephaloglycine
(6R)-3-acetoxymethyl-7t-((R)-2-amino-2-phenyl-acetylamino)-8-oxo-(6rH)-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Cephaoglycin acid
(6R,7R)-3-(acetyloxymethyl)-7-[[(2R)-2-amino-2-phenylacetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Cefaloglycine
Cefaloglicina
CEPHALOGLYCIN
D-Cephaloglycine
Kafocin
Cefaloglycinum
Cephaloglycin anhydrous
描述 Cefaloglycin (Cephaloglycin) 是一种具有口服活性的肾毒性 β-内酰胺类 (β-lactam) 头孢菌素抗生素,具有抗菌活性。Cefaloglycin 对肠球菌以外的革兰氏阳性球菌 (Gram-Positive cocci) 有活性。Cefaloglycin 对线粒体底物的摄取和呼吸也具有毒性。
相关类别
靶点

Gram-Positive cocci[2]

体外研究 头孢克洛在体外抗化脓链球菌的活性方面与头孢菌素相当,并略优于头孢氨苄[2]。
体内研究 在每毫升暴露2至6小时至300至3000微克头孢甘氨酸(头孢甘氨酸)的兔肾皮质线粒体中,测量琥珀酸盐和ADP的呼吸和摄取,然后清洗以去除抗生素。头孢菌素(Cefaloglycin)不可逆地降低呼吸和琥珀酸摄取。头孢氨苄对线粒体底物摄取和呼吸的体外损伤模式具有时间依赖性和浓度依赖性[1]。
参考文献

[1]. B M Tune, et al. The Renal Mitochondrial Toxicity of Beta-Lactam Antibiotics: In Vitro Effects of Cephaloglycin and Imipenem. J Am Soc Nephrol. 1990 Nov;1(5):815-21.

[2]. S Shadomy, et al. In Vitro Activities of Five Oral Cephalosporins Against Aerobic Pathogenic Bacteria. Antimicrob Agents Chemother. 1977 Nov;12(5):609-13.

[3]. E Bergogne-Bérézin. Continuous Activity of Significant Antibiotics. Clin Ther. Jan-Feb 1991;13(1):181-8.

密度 1.52 g/cm3
沸点 761.8ºC at 760mmHg
熔点 236.5°C (rough estimate)
分子式 C18H19N3O6S
分子量 405.42500
闪点 414.5ºC
精确质量 405.09900
PSA 164.33000
LogP 1.01720
折射率 1.678
储存条件 库房通风低温干燥

CHEMICAL IDENTIFICATION

RTECS NUMBER :
XI0345000
CHEMICAL NAME :
5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-(2-amino-2-phenylacetamido)- 3-(hydroxymethyl)-8-oxo-, acetate (ester), D-
CAS REGISTRY NUMBER :
3577-01-3
LAST UPDATED :
199603
DATA ITEMS CITED :
8
MOLECULAR FORMULA :
C18-H19-N3-O6-S
MOLECULAR WEIGHT :
405.46
WISWESSER LINE NOTATION :
T46 ANV EM GUTJ CMVYZR& G1OV1 HVQ

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 :
>10 gm/kg
TOXIC EFFECTS :
Liver - 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: 18,22,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1300 mg/kg
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 18,22,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
2800 mg/kg
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 18,22,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>10 gm/kg
TOXIC EFFECTS :
Liver - 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: 18,22,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1030 mg/kg
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 18,22,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
3700 mg/kg
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 18,22,1970 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1200 mg/kg
SEX/DURATION :
female 9-14 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced 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: 18,39,1970
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
12 gm/kg
SEX/DURATION :
female 7-12 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 18,39,1970

危害码 (欧洲) Xn
风险声明 (欧洲) 42/43
安全声明 (欧洲) 36

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3577-01-3结构式

3577-01-3

文献:Ogasa; Saito; Hashimoto; Sato; Hirata Chemical and Pharmaceutical Bulletin, 1989 , vol. 37, # 2 p. 315 - 321

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3577-01-3结构式

3577-01-3

文献:Spencer; Flynn; Roeske; Siu; Chauvette Journal of medicinal chemistry, 1966 , vol. 9, # 5 p. 746 - 750

~%

3577-01-3结构式

3577-01-3

文献:Spencer; Flynn; Roeske; Siu; Chauvette Journal of medicinal chemistry, 1966 , vol. 9, # 5 p. 746 - 750

~%

3577-01-3结构式

3577-01-3

文献:Kawamori; Hashimoto; Katsumata; et al. Agricultural and Biological Chemistry, 1983 , vol. 47, # 11 p. 2503 - 2509