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盐酸壮观霉素,五水合物

盐酸壮观霉素,五水合物用途

Spectinomycin dihydrochloride pentahydrate是广谱的氨基环糊精抗生素,可以抑制多种革兰氏阳性和革兰氏阴性生物的生长。

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盐酸壮观霉素,五水合物名称

[ CAS 号 ]:
22189-32-8

[ 中文名 ]:
大观霉素二盐酸盐五水合物

[ 英文名 ]:
Spectinomycin dihydrochloride pentahydrate

[中文别名 ]:

[英文别名 ]:

MFCD00150886
spectogard
EINECS 244-554-3
Spectinomycin pentahydrate dihydrochloride
ACTINOSPECTACIN DIHYDROCHLORIDE
Spectinomycin HCL USP/BP
Spectinomycin dihydrochloride pentahydrate
SPECTINOMYCIN 2HCL
Trobicin (tn)
SPECTINOMYCIN HCL

盐酸壮观霉素,五水合物生物活性

[ 描述 ]:

Spectinomycin dihydrochloride pentahydrate是广谱的氨基环糊精抗生素,可以抑制多种革兰氏阳性和革兰氏阴性生物的生长。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌

研究领域 >> 感染

[体外研究]

大观霉素选择性抑制细胞和大肠杆菌提取物中的蛋白质合成。当添加到指数生长的培养物中时,壮观霉素(50μg/ mL)快速且可逆地抑制大肠杆菌的生长。氨基酸掺入立即减慢,但RNA合成继续进行。在大肠杆菌B的提取物中,壮观霉素抑制由内源信使RNA或MS-2噬菌体RNA指导的多肽合成。在1μg/ mL(3μM)下实现最大抑制(70至80％)。 [1]。大观霉素通过抑制延伸因子G与核糖体的结合来阻断肽基-tRNA从A位点向P位点的易位。大观霉素与16S rRNA中的残基G1064和01192特异性相互作用,并可能将该分子转变为无活性构象[2]。壮观霉素作为td内含子RNA的混合非竞争性抑制剂,Ki为7.2mM。大观霉素的剪接抑制依赖于pH变化和Mg2 +浓度,表明与内含子RNA的静电相互作用[3]。

[体内研究]

肾脏排泄是壮观霉素的主要消除途径。 IV给药后,约55％的药物以未改变的形式排泄到尿液中。静脉内施用10mg/kg壮观霉素后,血浆峰浓度为37.8μg/ mL,全身暴露(曲线下面积AUC0-∞)为15.7μg/ mL。单剂量肌内给药后,壮观霉素的整体消除半衰期为牛1.2小时,绵羊1.0小时,猪1.0小时,鸡肉1.65小时,人类1.85小时[4]。

[动物实验]

大鼠：对大鼠静脉内施用壮观霉素（10mg / kg）。在给药前和给药后0.25,0.5,0.75,1.0,1.5,2.0,4.0,6.0,8.0,12.0,24.0,36.0和48.0小时收集连续血液样品（约250μL）。通过离心（10,000g在4℃下5分钟）立即分离血浆并储存在-80℃直至分析。在给药后0-6,6-12,12-24,24-36和36-48小时的间隔收集尿液样品并储存在-80℃直至分析[4]。

[参考文献]

[1]. Davies J, et al. Inhibition of protein synthesis by spectinomycin. Science. 1965 Sep 3;149(3688):1096-8.

[2]. Brink MF, et al. Spectinomycin interacts specifically with the residues G1064 and C1192 in 16S rRNA, thereby potentially freezing this molecule into an inactive conformation. Nucleic Acids Res. 1994 Feb 11;22(3):325-31.

[3]. Park IK, et al. Spectinomycin inhibits the self-splicing of the group 1 intron RNA. Biochem Biophys Res Commun. 2000 Mar 16;269(2):574-9.

[4]. Madhura DB, et al. Pharmacokinetic profile of spectinomycin in rats. Pharmazie. 2013 Aug;68(8):675-6.

[相关活性小分子]

盐酸壮观霉素,五水合物物理化学性质

[ 沸点 ]:
583.1ºC at 760 mmHg

[ 熔点 ]:
205-207° (dec)

[ 分子式 ]:
C₁₄H₃₆Cl₂N₂O₁₂

[ 分子量 ]:
495.348

[ 闪点 ]:
306.4ºC

[ 精确质量 ]:
494.164520

[ PSA ]:
175.66000

[ 外观性状 ]:
一种圆形的无色晶体

[ 蒸汽压 ]:
5.05E-16mmHg at 25°C

[ 储存条件 ]:
2~8°C

盐酸壮观霉素,五水合物MSDS

详细MSDS(安全技术说明书)

盐酸壮观霉素,五水合物毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: WG7400000

CHEMICAL NAME :: Spectinomycin, dihydrochloride, pentahydrate

CAS REGISTRY NUMBER :: 22189-32-8

LAST UPDATED :: 199706

DATA ITEMS CITED :: 13

MOLECULAR FORMULA :: C14-H24-N2-O7.2Cl-H.5H2-O

MOLECULAR WEIGHT :: 494.41

WISWESSER LINE NOTATION :: T C666 BO DO GV IOTJ E1 HQ KM1 LQ MM1 NQ &GH 2 &QH 5

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 :: >5 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

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: 29,43,1976

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2020 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

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: 29,43,1976

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

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: 29,43,1976

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2500 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

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: 29,43,1976

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

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: 29,43,1976

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2350 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

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: 29,43,1976

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 8400 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

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: 29,43,1976

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

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: 29,43,1976 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 6800 mg/kg/39D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - other changes

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: 29,43,1976

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2800 mg/kg/32D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Endocrine - changes in adrenal weight

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: 29,43,1976 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 2400 mg/kg

SEX/DURATION :: female 9-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 8,3018,1974

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 2400 mg/kg

SEX/DURATION :: female 7-12 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - eye/ear

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 8,3008,1974 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X6089 No. of Facilities: 17 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 958 (estimated) No. of Female Employees: 434 (estimated)

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盐酸壮观霉素,五水合物安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
T+

[ 安全声明 (欧洲) ]:
24/25

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

[ WGK德国 ]:
2

[ RTECS号 ]:
WG7400000

[ 海关编码 ]:
29419090

盐酸壮观霉素,五水合物制备

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盐酸壮观霉素,五水合物文献

Aminoglycoside analysis in food of animal origin with a zwitterionic stationary phase and liquid chromatography-tandem mass spectrometry.

Anal. Chim. Acta 882 , 127-39, (2015)

In this study, fourteen highly polar aminoglycoside (AGs) antibiotics were selected. Various stationary phases were tested, including Obelisc R, ZIC-HILIC, BEH amide and aminopropyl. The nature of the...

DrugBank 3.0: a comprehensive resource for 'omics' research on drugs.

Nucleic Acids Res. 39 , D1035-41., (2011)

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Molecular epidemiology of Neisseria gonorrhoeae isolates from Saskatchewan, Canada: utility of NG-MAST in predicting antimicrobial susceptibility regionally.

Sex. Transm. Infect. 90(4) , 297-302, (2014)

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盐酸壮观霉素,五水合物

盐酸壮观霉素,五水合物用途

盐酸壮观霉素,五水合物名称

盐酸壮观霉素,五水合物生物活性

盐酸壮观霉素,五水合物物理化学性质

盐酸壮观霉素,五水合物MSDS

详细MSDS(安全技术说明书)

盐酸壮观霉素,五水合物毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

盐酸壮观霉素,五水合物安全信息

盐酸壮观霉素,五水合物制备

盐酸壮观霉素,五水合物文献

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