|
Spectinomycin (dihydrochloride) | 盐酸大观霉素
MCE 国际站:Spectinomycin (dihydrochloride)
中文名:盐酸大观霉素
CAS:21736-83-4
品牌:MedChemExpress (MCE)
存储条件:4°C, sealed storage, away from moisture
生物活性:Spectinomycin dihydrochloride 是一种广谱抗生素,可抑制多种革兰氏阳性和革兰氏阴性菌的生长。 Spectinomycin dihydrochloride 通过选择性靶向细菌 核糖体并中断蛋白质合成发挥作用。 Spectinomycin dihydrochloride 也是 td 内含子 RNA 的非竞争性抑制剂,Ki 值为 7.2 mM[1]-[5]。 IC50 和靶标:细菌核糖体亚基[5]
体外 :大观霉素二盐酸盐选择性抑制细胞和大肠杆菌提取物中的蛋白质合成大肠杆菌:Spectinomycin dihydrochloride (50 μg/mL) 快速且可逆地抑制Escherichia coli 生长,并立即抑制氨基酸掺入[1]。Spectinomycin dihydrochloride(1 μg/mL 或 3 μM)抑制由内源信使 RNA 或 MS-2 噬菌体 RNA 指导的多肽合成,在 Escherichia coli[1][1].大观霉素二盐酸盐通过抑制延伸因子 G 与核糖体[2].Spectinomycin dihydrochloride 与 16S rRNA 中的残基 G1064 和 01192 特异性相互作用,并可能使其失活[2].Spectinomycin二盐酸ide 表现出剪接抑制并依赖于 pH 变化和 Mg2+ 浓度,表明与内含子 RNA[3] 的静电相互作用。
体内:Spectinomycin dihydrochloride (20 mg/kg; im; 20-100 mg/kg; 9 d) 在健康雏鸡中表现出安全性[4]。Spectinomycin dihydrochloride (10 mg/kg; iv ;单次给药)主要通过肾脏排泄消除途径,约55%以原形从尿中排泄[5].大观霉素二盐酸盐在大鼠体内的药代动力学[5]
参数 | C0 (μg/mL) | AUC0-∞ (μg•h/mL) | Vd (L/kg) | CL (L/h/kg) | MRT (h) | T1/2α (h) | T1/2β (h) | T1/2γ (h) | fe | CL肾 (L/h/kg) | Eratio |
非房室分析 | 44.3 | 16.8 | 0.756 | 0.602 | 0.757 | / | / | / | 0.553 | 0.359 | 1.00 |
三隔间模型 | 37.8 | 15.7 | 0.747 | 0.649 | 1.11 | / | 0.237 | 0.754 | 19.5 | / | / |
热销产品:Efavirenz | Pyrroloquinoline quinone (disodium salt) | Daxdilimab | GSK467 | 5-FAM | Peimine | KR-33493 | DCZ0415 | Caffeic acid | Halicin
研究领域:Anti-infection
作用靶点:Bacterial | Antibiotic
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
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]. Khan EA, et al. Safety evaluation study of lincomycin and spectinomycin hydrochloride intramuscular injection in chickens. Toxicol Rep. 2022 Jan 29;9:204-209.
[5]. Madhura DB, et al. Pharmacokinetic profile of spectinomycin in rats. Pharmazie. 2013 Aug;68(8):675-6.
Archiver|手机版|科学网 ( 京ICP备07017567号-12 )
GMT+8, 2024-8-22 13:45
Powered by ScienceNet.cn
Copyright © 2007- 中国科学报社