Spectinomycin sulfate hydrate | MedChemExpress (MCE)
产品名称: Spectinomycin sulfate hydrate | MedChemExpress (MCE)
英文名称: Spectinomycin sulfate hydrate
产品编号: HY-W928617
产品价格: 0
产品产地: 美国
品牌商标: MedChemExpress (MCE)
更新时间: 2024-07-30T10:43:54
使用范围: null
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Spectinomycin sulfate hydrate
CAS No. : 64058-48-6
MCE 国际站:Spectinomycin sulfate hydrate
产品活性:Spectinomycin sulfate hydrate 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 sulfate hydrate 通过特异靶向细菌核糖体,干扰蛋白质合成。Spectinomycin sulfate hydrate 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:Antibiotic | Bacterial
In Vitro: Spectinomycin sulfate hydrate selectively inhibits protein synthesis in cells and in extracts of Escherichia coli:
Spectinomycin sulfate hydrate (50 μg/mL) inhibits Escherichia coli growth rapidly and reversibly, and suppresses amino acid incorporation immediately.
Spectinomycin sulfate hydrate (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 sulfate hydrate blocks the translocation of peptidyl-tRNAs from A-site to P-site by inhibiting the binding of elongation factor G to the ribosome.
Spectinomycin sulfate hydrate interacts specifically with the residues G1064 and 01192 in 16S rRNA and potentially makes it inactive.
Spectinomycin sulfate hydrate exhibits splicing inhibition and is dependent on pH changes and Mg2+ concentration, indicating electrostatic interactions with the intron RNA.
In Vivo: Spectinomycin dihydrochloride pentahydrate (20 mg/kg; i.m.; 20-100 mg/kg; 9 d) shows the safety in healthy chicks.
Spectinomycin dihydrochloride pentahydrate (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 pentahydrate 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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