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金霉素

金霉素用途

Chlortetracycline (7-Chlorotetracycline) 是一种特异性的有效钙离子载体抗生素, 抑制氨酰 tRNA 结合到核糖体。

金霉素名称

[ CAS 号 ]:
57-62-5

[ 中文名 ]:
氯四环素

[ 英文名 ]:
Chlortetracycline

[中文别名 ]:

金霉素

[英文别名 ]:

Aurofac
auromycin
Aurofac 10
Duomycin
Orospray
Centraureo
EINECS 200-341-7
Chrysomykine
Uromycin
Acronize

金霉素生物活性

[ 描述 ]:

Chlortetracycline (7-Chlorotetracycline) 是一种特异性的有效钙离子载体抗生素, 抑制氨酰 tRNA 结合到核糖体。

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[参考文献]

[1]. Elmund GK, et al. Role of excreted chlortetracycline in modifying the decomposition process in feedlot waste. Bull Environ Contam Toxicol. 1971 Mar-Apr;6(2):129-32.

[2]. Saling PM, et al. Mouse gamete interactions during fertilization in vitro. Chlortetracycline as a fluorescent probe for the mouse sperm acrosome reaction. J Cell Biol. 1979 Dec;83(3):544-55.

金霉素物理化学性质

[ 密度 ]:
1.7±0.1 g/cm3

[ 沸点 ]:
821.1±65.0 °C at 760 mmHg

[ 熔点 ]:
168.5ºC

[ 分子式 ]:
C₂₂H₂₃ClN₂O₈

[ 分子量 ]:
478.880

[ 闪点 ]:
450.4±34.3 °C

[ 精确质量 ]:
478.114288

[ PSA ]:
181.62000

[ LogP ]:
-0.53

[ 外观性状 ]:
金色黄色晶体粉末

[ 蒸汽压 ]:
0.0±3.1 mmHg at 25°C

[ 折射率 ]:
1.745

[ 储存条件 ]:
2-8°C

金霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QI7750000

CHEMICAL NAME :: 2-Naphthacenecarboxamide, 7-chloro-4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octah ydro- 3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-

CAS REGISTRY NUMBER :: 57-62-5

LAST UPDATED :: 199701

DATA ITEMS CITED :: 17

MOLECULAR FORMULA :: C22-H23-Cl-N2-O8

MOLECULAR WEIGHT :: 478.92

WISWESSER LINE NOTATION :: L E6 C666 BV FV CU GUTTT&J DQ EQ GVZ HQ IN1&1 MQ M1 OG RQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3 gm/kg

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

REFERENCE :: JAFCAU Journal of Agricultural and Food Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB 57136, West End Stn., Washington, DC 20037) V.1- 1953- Volume(issue)/page/year: 17,497,1969

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 335 mg/kg

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

REFERENCE :: CLDND* Compilation of LD50 Values of New Drugs. (J.R. MacDougal, Dept. of National Health and Welfare, Food and Drug Divisions, 35 John St., Ottawa, Ont., Canada)

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 118 mg/kg

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

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 6,623,1956

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1500 mg/kg

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

REFERENCE :: AAGAAW Antimicrobial Agents Annual. (New York, NY) 1960. For publisher information, see AMACCQ. Volume(issue)/page/year: -,595,1960

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 192 mg/kg

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

REFERENCE :: CLDND* Compilation of LD50 Values of New Drugs. (J.R. MacDougal, Dept. of National Health and Welfare, Food and Drug Divisions, 35 John St., Ottawa, Ont., Canada)

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3 gm/kg

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

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 6,623,1956

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 134 mg/kg

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

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 6,623,1956

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

ROUTE OF EXPOSURE :: Intracerebral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 48 mg/kg

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions Behavioral - excitement Musculoskeletal - changes in teeth and supporting structures

REFERENCE :: CHTHBK Chemotherapy (Basel). (S. Karger Pub., Inc., 79 Fifth Ave., New York, NY 10003) V.13- 1968- Volume(issue)/page/year: 26,196,1980

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 750 mg/kg

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

REFERENCE :: AAGAAW Antimicrobial Agents Annual. (New York, NY) 1960. For publisher information, see AMACCQ. Volume(issue)/page/year: -,595,1960

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 150 mg/kg

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

REFERENCE :: HBTXAC "Handbook of Toxicology," 4 vols., Philadelphia, W.B. Saunders Co., 1956-59 Volume(issue)/page/year: 5,52,1959

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 1800 mg/kg

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

REFERENCE :: ANTBAL Antibiotiki. (Moscow, USSR) V.1-29, 1956-84. For publisher information, see AMBIEH. Volume(issue)/page/year: 20,793,1975 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2500 mg/kg/5D-I

TOXIC EFFECTS :: Liver - change in gall bladder structure or function Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

REFERENCE :: ANTBAL Antibiotiki. (Moscow, USSR) V.1-29, 1956-84. For publisher information, see AMBIEH. Volume(issue)/page/year: 28,608,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 6 gm/kg/30D-I

TOXIC EFFECTS :: Gastrointestinal - other changes Kidney, Ureter, Bladder - other changes in urine composition Immunological Including Allergic - decreased immune response

REFERENCE :: ANTBAL Antibiotiki. (Moscow, USSR) V.1-29, 1956-84. For publisher information, see AMBIEH. Volume(issue)/page/year: 20,793,1975 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 372 mg/kg

SEX/DURATION :: female 1-6 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

REFERENCE :: ASPHAK Archives des Sciences Physiologique. (Paris, France) V.1-28, 1947-74. Discontinued. Volume(issue)/page/year: 23,481,1969 *** OCCUPATIONAL EXPOSURE LIMITS *** OEL-RUSSIA:STEL 0.1 mg/m3;Skin JAN 1993 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5542 No. of Facilities: 921 (estimated) No. of Industries: 3 No. of Occupations: 17 No. of Employees: 12911 (estimated) No. of Female Employees: 125 (estimated)

金霉素安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R22

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

[ RTECS号 ]:
QI7750000

金霉素合成路线

详细合成路线

金霉素上下游产品

金霉素上游产品

金霉素下游产品

金霉素制备

1.由金色链霉菌（Streptomyces aureofacieus）发酵产生，发酵液经酸化、过滤得沉淀物，溶解于乙醇后经酸析得粗品，经溶解、成盐得盐酸盐结晶。

2.由金色链霉菌发酵产生，发酵经酸化、过滤得沉淀物，溶解于乙醇后经酸析得粗品，再进行溶解、成盐得其盐酸盐结晶。

金霉素文献

Metagenome-wide association of microbial determinants of host phenotype in Drosophila melanogaster.

MBio 5(5) , e01631-14, (2014)

Animal-associated bacteria (microbiota) affect host behaviors and physiological traits. To identify bacterial genetic determinants of microbiota-responsive host traits, we employed a metagenome-wide a...

Photolysis of chlortetracycline in aqueous solution: kinetics, toxicity and products.

J. Environ. Sci. (China) 24(2) , 254-60, (2012)

The aqueous photodegradation of the widely used antibiotic chlortetracycline (CTC) was investigated under simulated sunlight. The quantum yield of photodegradation increased from 3.3 x 10(-4) to 8.5 x...

Validation of Polo-like kinase 1 as a therapeutic target in pancreatic cancer cells.

Cancer Biol. Ther. 13(12) , 1214-20, (2012)

Polo-like kinase 1 (PLK1) is a serine/threonine protein kinase and plays a critical role in mitosis. PLK1 has also been regarded as a valuable target for cancer treatment, and several PLK1 inhibitors ...

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金霉素