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CAS No. : 21736-83-4
MCE 国际站:Spectinomycin dihydrochloride
产品活性:Spectinomycin dihydrochloride 是一种广谱抗生素,可以抑制多种革兰氏阳性和革兰氏阴性细菌的生长。Spectinomycin dihydrochloride 通过特异靶向细菌核糖体,干扰蛋白质合成。Spectinomycin dihydrochloride 也是 td 内含子 RNA 的非竞争性抑制剂,Ki 为 7.2 mM。
研究领域:Anti-infection
作用靶点:Bacterial | Antibiotic
结构分类:抗生素 | 疾病研究 | 抗菌 | 抗生素 | 其他类 | 抗生素 | 哺乳动物细胞培养 | 抗生素 | 抗性筛选 | 结构分类
In Vitro: Spectinomycin dihydrochloride selectively inhibits protein synthesis in cells and in extracts of Escherichia coli:
Spectinomycin dihydrochloride (50 μg/mL) inhibits Escherichia coli growth rapidly and reversibly, and suppresses amino acid incorporation immediately.
Spectinomycin dihydrochloride (1 μg/mL or 3 μM) inhibits polypeptide synthesis directed either by endogenous messenger RNA or by MS-2 bacteriophage RNA, with maximum inhibition of 70-80% in extracts of Escherichia coli.
Spectinomycin dihydrochloride blocks the translocation of peptidyl-tRNAs from A-site to P-site by inhibiting the binding of elongation factor G to the ribosome.
Spectinomycin dihydrochloride interacts specifically with the residues G1064 and 01192 in 16S rRNA and potentially makes it inactive.
Spectinomycin dihydrochloride exhibits splicing inhibition and dependent on pH changes and Mg2+ concentration, indicating electrostatic interactions with the intron RNA.
In Vivo: Spectinomycin dihydrochloride (20 mg/kg; i.m.; 20-100 mg/kg; 9 d) shows the safety in healthy chicks.
Spectinomycin dihydrochloride (10 mg/kg; i.v.; single dose) has the major elimination pathway by renal excretion, approximately 55% is excreted into the urine in unchanged form.
Pharmacokinetics of Spectinomycin dihydrochloride in Rat
Parameter | 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 | CLrenal (L/h/kg) | Eratio |
Non atrioventricular analysis | 44.3 | 16.8 | 0.756 | 0.602 | 0.757 | / | / | / | 0.553 | 0.359 | 1.00 |
Three-compartment model | 37.8 | 15.7 | 0.747 | 0.649 | 1.11 | / | 0.237 | 0.754 | 19.5 | / | / |
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