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66803-19-8

66803-19-8结构式
66803-19-8结构式
  • 常用中文名:硫酸小诺霉素
  • 常用英文名:Micronomicin sulfate
  • CAS号:66803-19-8
  • 分子式:C20H41N5O7.xH2O4S
  • 分子量:561.647
  • 相关类别: 原料药 抗生素类药物 氨基糖苷类药
  • 发布时间:2018-02-16 08:00:00
  • 更新时间:2024-01-09 15:28:37
  • Micronomicin sulfate (Gentamicin C2b sulfate) 是从 Micromonospora 中分离出来的氨基糖苷抗生素 (antibiotic)。Micronomicin sulfate 是一种接近庆大霉素类抗生素的广谱抗生素,对假单胞菌、变形杆菌、肺炎克雷伯菌、沙雷菌等具有高的抑制活性 (MIC=0.001-8.3 μg/ml)。

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中文名 硫酸小诺霉素
英文名 (2R,3R,4R,5R)-2-[(1S,2S,3R,4S,6R)-4,6-diamino-3-[(2R,3R,6S)-3-amino-6-(methylaminomethyl)oxan-2-yl]oxy-2-hydroxycyclohexyl]oxy-5-methyl-4-(methylamino)oxane-3,5-diol,sulfuric acid
中文别名 沙加霉素
英文别名 α-D-erythro-Hexopyranoside, (1R,2S,3S,4R,6S)-4,6-diamino-3-[[3-deoxy-4-C-methyl-3-(methylamino)-β-L-arabinopyranosyl]oxy]-2-hydroxycyclohexyl 2-amino-2,3,4,6-tetradeoxy-6-(methylamino)-, sulfate (1:1) (salt)
α-D-erythro-Hexopyranoside, (1R,2S,3S,4R,6S)-4,6-diamino-3-[[3-deoxy-4-C-methyl-3-(methylamino)-β-L-arabinopyranosyl]oxy]-2-hydroxycyclohexyl 2-amino-2,3,4,6-tetradeoxy-6-(methylamino)-, sulfat e (1:1) (salt)
(1R,2S,3S,4R,6S)-4,6-Diamino-3-{[3-deoxy-4-C-methyl-3-(methylamino)-β-L-arabinopyranosyl]oxy}-2-hydroxycyclohexyl 2-amino-2,3,4,6-tetradeoxy-6-(methylamino)-α-D-erythro-hexopyranoside sulfate ( 1:1)
(1R,2S,3S,4R,6S)-4,6-Diamino-3-{[3-deoxy-4-C-methyl-3-(methylamino)-β-L-arabinopyranosyl]oxy}-2-hydroxycyclohexyl 2-amino-2,3,4,6-tetradeoxy-6-(methylamino)-α-D-erythro-hexopyranoside sulfate (1:1)
Micronomycin sulfate
micronomicin sulfate
Sagamacin
描述 Micronomicin sulfate (Gentamicin C2b sulfate) 是从 Micromonospora 中分离出来的氨基糖苷抗生素 (antibiotic)。Micronomicin sulfate 是一种接近庆大霉素类抗生素的广谱抗生素,对假单胞菌、变形杆菌、肺炎克雷伯菌、沙雷菌等具有高的抑制活性 (MIC=0.001-8.3 μg/ml)。
相关类别
靶点

MIC: 0.001-8.3 μg/ml (Pseudomonas, Proteus, Klebsiella pneumoniae, Serratia)[2]

体外研究 小诺霉素具有很强的抗菌活性,对金黄色葡萄球菌FDA 209 P、金黄色葡萄球菌最低抑菌值为0.01μg/ml,对大肠杆菌St.M.589、Baker 2、F 14-BK和R5/W677也有活性,最小抑菌值为0.75μg/ml、0.3μg/ml、0.03μg/ml和0.03μg/ml它对铜绿假单胞菌株和肺炎列巴耶拉菌株(MICs=0.03-17.5μg/ml)具有活性[1]。
体内研究 硫酸小诺霉素对小鼠的各种细菌感染具有高度的活性,在小鼠体内的急性LD50为93 mg/kg[1]。注射硫酸小诺霉素(静脉注射;4-100 mg/kg;30天)用于亚急性毒性研究。wistar大鼠在100 mg/kg的剂量水平下死亡(30只动物中有10只):肾脏疾病和共济失调。肾组织学紊乱主要发生在25mg/kg及以上的剂量水平[3]。动物模型:Wistar大鼠[3]剂量:4,10,25,63mg/kg和100mg/kg给药:静脉注射;30天结果:100mg/kg导致大鼠死亡。
参考文献

[1]. R Okachi,et al. A New Antibiotic XK-62-2 (Sagamicin). I. Isolation, Physicochemical and Antibacterial Properties. J Antibiot (Tokyo)

[2]. P J Daniels, The Gentamicin Antibiotics. 6. Gentamicin C2b, an Aminoglycoside Antibiotic Produced by Micromonospora Purpurea Mutant JI-33. J Antibiot (Tokyo)

[3]. T Hara, et al. Safety Evaluation of Micronomicin V. Subacute Toxicity in Rats After Intravenous Injection. Jpn J Antibiot. 1983 Nov;36(11):3208-25.

密度 1.32g/cm3
沸点 667.2ºC at 760mmHg
分子式 C20H41N5O7.xH2O4S
分子量 561.647
闪点 357.3ºC
精确质量 561.268005
PSA 282.71000
储存条件 2-8°C,干燥

CHEMICAL IDENTIFICATION

RTECS NUMBER :
WK2196000
CHEMICAL NAME :
Streptamine, O-2-amino-2,3,4,6-tetradeoxy-6-(methylamino)-alpha-D- erythro-hexopyranosyl- (1-4)-O-(3-deoxy-4-C-methyl-3-(methylamino)-beta-L-ar abinopyranosyl-(1-6)) -2-deoxy-, sulfate, D-
CAS REGISTRY NUMBER :
66803-19-8
LAST UPDATED :
199806
DATA ITEMS CITED :
9
MOLECULAR FORMULA :
C21-H43-N5-O6.H2-O4-S
MOLECULAR WEIGHT :
559.77
WISWESSER LINE NOTATION :
T6OTJ CZ F1M1 BO- BL6TJ AZ CQ EZ DO- BT6OTJ CQ DM1 EQ E1

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 :
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: -,1323,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1223 mg/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-18,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
104 mg/kg
TOXIC EFFECTS :
Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - cyanosis
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 36,3204,1983
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
625 mg/kg
TOXIC EFFECTS :
Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - cyanosis
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 36,3204,1983
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
15600 mg/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: -,1323,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
350 mg/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-18,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
245 mg/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-18,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
459 mg/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-18,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
459 mg/kg
TOXIC EFFECTS :
Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory stimulation Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 36,3204,1983

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