CAS |
No.39831-55-5 |
中文名称 |
硫酸阿米卡星 |
英文名称 |
Amikacin Sulfate |
别名 |
BAY-416651 sulfate;BB-K8;Pierami;阿米卡星硫酸盐 |
分子式 |
C22H43N5O13·2H2SO4 |
分子量 |
781.76 |
溶解性 |
Soluble in Water ≥10mg/mL |
酶活/效价 |
674-786μg/mg |
外观(性状) |
White to off-white Solid |
储存条件 |
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
EC |
EINECS 254-648-6 |
MDL |
MFCD00167475 |
SMILES |
OS(O)(=O)=O.OS(O)(=O)=O.O[C@@H]1[C@H]([C@@H](C[C@H](N)[C@H]1O[C@@]([C@@H]([C@@H](O)[C@@H]2O)O)([H])O[C@@H]2CN)NC([C@@H](O)CCN)=O)O[C@@]([C@@H]([C@@H](N)[C@@H]3O)O)([H])O[C@@H]3CO |
InChIKey |
FXKSEJFHKVNEFI-GCZBSULCSA-N |
InChI |
InChI=1S/C22H43N5O13.2H2O4S/c23-2-1-8(29)20(36)27-7-3-6(25)18(39-22-16(34)15(33)13(31)9(4-24)37-22)17(35)19(7)40-21-14(32)11(26)12(30)10(5-28)38-21;2*1-5(2,3)4/h6-19,21-22,28-35H,1-5,23-26H2,(H,27,36);2*(H2,1,2,3,4)/t6-,7+,8-,9+,10+,11-,12+,13+,14+,15-,16+,17-,18+,19-,21+,22+;;/m0../s1 |
PubChem CID |
38351 |
靶点 |
Bacterial |
通路 |
Anti-infection |
背景说明 |
是一种氨基糖苷类抗生素。具有杀菌作用,作用于细菌核糖体的30S亚单位,抑制细菌合成蛋白质,对多数肠杆菌科细菌具良好作用。 |
生物活性 |
Amikacin disulfate (BAY 41-6551 dissulfate) is an aminoglycoside antibiotic and a semisynthetic analog of kanamycin. Amikacin disulfate is bactericidal, acting directly on the 30S and 50S bacerial ribosomal subunits to inhibit protein synthesis. Amikacin disulfate is very active against most Gram-negative bacteria including gentamicin- and tobramycin-resistant strains. Amikacin disulfate also inhibits the infections caused by susceptible Nocardia and nontuberculous mycobacteria[1-2]. |
In Vitro |
Amikacin offers definite advantages for treating infections caused by organisms resistant to other aminoglycosides. Amikaci is affected by relatively few arninoglycoside-modifying enzymes. Amikacin is useful in the treatment of infections caused by Nocardia asteroides,Mycobacterium avium-intracellulare,and certain species of rapid-growing mycobacteria(that is,M. chelonae and M. fortuitumi)[1].Amikacin(100-1500 μM)causes a reliable dose-dependent loss of lateral line zebrafish hair cells with a LD50 value of 453 μM[3]. |
In Vivo |
Amikacin(320mg/kg; subcutaneous injection; daily; for 10 days; male Fischer rats)treatment increases the chance of serious hearing loss in rats in vivo[3]. |
动物实验 |
Animal Model: Male Fischer 344 rats(40-50-day-old);Dosage: 320 mg/kg;Administration: Subcutaneous injection; daily; for 10 days[3] |
数据来源文献 |
[1]. Edson, R.S. and C.L. Terrell, The aminoglycosides. Mayo Clin Proc, 1999. 74(5): p. 519-28. [2]. Ristuccia AM, et al. An overview of amikacin. Ther Drug Monit. 1985;7(1):12-25. [3]. Sian R Kitcher, et al. ORC-13661 Protects Sensory Hair Cells From Aminoglycoside and Cisplatin Ototoxicity. JCI Insight. 2019 Aug 8;4(15):e126764. |
规格 |
100mg 500mg 1g |
单位 |
瓶 |