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Kasugamycin (hydrochloride)

盐酸春雷霉素
Catalog No.
C5503
氨基糖苷类抗生素
组合的产品项目
规格价格库存 数量
5g
¥ 1,867.00
Ship with 10-15 days
10g
¥ 2,777.00
Ship with 10-15 days

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A

背景

Kasugamycin is an aminoglycosidic antibiotic.

Aminoglycoside, a medicinal and bacteriologic category of traditional Gram-negative antibacterial therapeutic agent, inhibits protein synthesis and contains as a portion of the molecule an amino-modified glycoside.

In vitro: Kasugamycin could inhibit protein synthesis by interacting with the 30S ribosomal subunit. The mechanism of inhibition of protein synthesis appeared to be different from that of other aminoglycosides, such as kanamycin, streptomycin, neomycin, gentamicin. The initiation complex formation on 30S ribosomes could be inhibited by kasugamycin but not by streptomycin, kanamycin or gentamicin, though the binding of fMet-tRNA to 70S ribosomes was inhibited by both streptomycin and by kasugamycin. [1].

In vivo: Five groups, each consisting of five guinea pigs, were infected with Shibaura strain; two groups were treated by injection with kasugamycin. All animals treated with 1 mcg/g were killed showing an average survival period of 7.4 days, which was close to the average survival period of 6.2 days in the control group; while all animals treated with 5 mcg/g survived. The other two groups were treated with kasugamycin from the icteric stage to the 10th day after infection. Two animals of the 5 mcg/g group survived, showing no leptospira in the kidney; the other three died in an average of 7.7 days. Three animals of the 10 mcg/g group survived; while the other two animals died in 6.5 days on an average . The total amounts of kasugamycin administered to the infected guinea pigs from the febrile stage were 10.8 mg (the 1 mcg/g group) and 54.0 mg (the 5 mcg/g group) [2].

Clinical trial: So far, no clinical study has been conducted.

References:
[1] Okuyama, A. ,Machiyama, N.,Kinoshita, T., et al. Inhibition by kasugamycin of initiation complex formation on 30S ribosomes. Biochemical and Biophysical Research Communications 43(1), 196-199 (1971).
[2] Kitaoka M, Mori M, Arimitsu Y.  In vitro and in vivo effects of kasugamycin on Leptospira icterohaemorrhagiae. Jpn J Med Sci Biol. 1975 Oct-Dec;28(5-6):285-90.

化学属性

StorageStore at -20°C
M.Wt415.8
Cas No.19408-46-9
FormulaC14H25N3O9·HCl
Solubilityinsoluble in EtOH; insoluble in DMSO; ≥41.6 mg/mL in H2O with gentle warming
Chemical Name3-O-[2-amino-4-[(carboxyiminomethyl)amino]-2,3,4,6-tetradeoxy-α-D-arabino-hexopyranosyl]-D-chiro-inositol, monohydrochloride
SDFDownload SDF
Canonical SMILESO[C@H]1[C@@H](O)[C@H](O)[C@H](O)[C@@H](O[C@@]2([H])O[C@H](C)[C@@H](NC(C(O)=O)=N)C[C@@H]2N)[C@@H]1O.Cl
运输条件 蓝冰运输或根据您的需求运输。
一般建议不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

试验操作

细胞实验 [1]:

细胞系

黄疸出血群

溶解方法

在DMSO中的溶解度是<4.16mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

50μg/ml

应用

立刻或者24小时后向接种黄疸出血群的5管Korthof培养基中添加50μg/ml的Kasugamycin,钩端螺旋体的生长全部受到抑制,在孵育48小时后添加100μg/ml的Kasugamycin,虽然亚培养物持续显示负增长,但并非所有的培养物都能被抑制。其他菌株也获得了相似的结果。

动物实验 [1]:

动物模型

几内亚猪

剂量

1 μg/g, 5μg/g, 10 μg/g

应用

用1 μg/g治疗的所有动物均被杀死,显示出平均生存期为7.4天,这与对照组的平均生存期6.2天相近。而用5 μg / g处理的所有动物均存活。从黄疸期到感染后第10天,其他两组均进行kasugamycin治疗处理,5μg / g组的两只动物存活下来,肾脏没有钩端螺旋体。其他三只动物平均死亡为7.7天。10 μg / g组的三只动物存活了下来,而另外两只动物平均死亡为6.5天。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Kitaoka M, Mori M, Arimitsu Y. In vitro and in vivo effects of kasugamycin on Leptospira icterohaemorrhagiae. Jpn J Med Sci Biol. 1975 Oct-Dec;28(5-6):285-90. PubMed PMID: 1047116.

质量控制

质量控制和MSDS

批次:

化学结构

Kasugamycin (hydrochloride)