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编 号：F202865
分子式：C14H24N2O7
分子量：332.35
分子式：C14H24N2O7
分子量：332.35
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CAS No: 1695-77-8
产品详情
生物活性：
Spectinomycin is a broad-spectrum antibiotic and inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin acts by selectively targeting to the bacterial ribosome and interrupting protein synthesis. Spectinomycin is also a noncompetitive inhibitor of td intron RNA.
体内研究：
Spectinomycin (20 mg/kg; i.m.; 20-100 mg/kg; 9 d) shows the safety in healthy chicks.Spectinomycin (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 in RatParameterC0 (μg/mL)AUC0-∞ (μg?h/mL)Vd (L/kg)CL (L/h/kg)MRT (h)T1/2α (h)T1/2β (h)T1/2γ (h)feCLrenal (L/h/kg)Eratio
Non atrioventricular analysis44.316.80.7560.6020.757///0.5530.3591.00
Three-compartment model37.815.70.7470.6491.11/0.2370.75419.5//
Animal Model:Arbor Acres plus broiler chicks (15-day-old)
Dosage:20 mg/kg, 60 mg/kg, 100 mg/kg
Administration:Intramuscular injection (chest muscles); 9 days
Result:Showed biosecurity of 20 mg/kg by complete blood count, biochemical parameters, histopathological, clinical signs, body weight gain, and feed conversion ratio (FCR).Resulted minor toxicity of 60 mg/kg.
体外研究：
Spectinomycin selectively inhibits protein synthesis in cells and in extracts of Escherichia coli. Spectinomycin (50 μg/mL) inhibits Escherichia coli growth rapidly and reversibly, and suppresses amino acid incorporation immediately. Spectinomycin (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 blocks the translocation of peptidyl-tRNAs from A-site to P-site by inhibiting the binding of elongation factor G to the ribosome. Spectinomycin interacts specifically with the residues G1064 and 01192 in 16S rRNA and potentially makes it inactive.Spectinomycin exhibits splicing inhibition and dependent on pH changes and Mg2+ concentration, indicating electrostatic interactions with the intron RNA.
Spectinomycin is a broad-spectrum antibiotic and inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin acts by selectively targeting to the bacterial ribosome and interrupting protein synthesis. Spectinomycin is also a noncompetitive inhibitor of td intron RNA.
体内研究：
Spectinomycin (20 mg/kg; i.m.; 20-100 mg/kg; 9 d) shows the safety in healthy chicks.Spectinomycin (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 in RatParameterC0 (μg/mL)AUC0-∞ (μg?h/mL)Vd (L/kg)CL (L/h/kg)MRT (h)T1/2α (h)T1/2β (h)T1/2γ (h)feCLrenal (L/h/kg)Eratio
Non atrioventricular analysis44.316.80.7560.6020.757///0.5530.3591.00
Three-compartment model37.815.70.7470.6491.11/0.2370.75419.5//
Animal Model:Arbor Acres plus broiler chicks (15-day-old)
Dosage:20 mg/kg, 60 mg/kg, 100 mg/kg
Administration:Intramuscular injection (chest muscles); 9 days
Result:Showed biosecurity of 20 mg/kg by complete blood count, biochemical parameters, histopathological, clinical signs, body weight gain, and feed conversion ratio (FCR).Resulted minor toxicity of 60 mg/kg.
体外研究：
Spectinomycin selectively inhibits protein synthesis in cells and in extracts of Escherichia coli. Spectinomycin (50 μg/mL) inhibits Escherichia coli growth rapidly and reversibly, and suppresses amino acid incorporation immediately. Spectinomycin (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 blocks the translocation of peptidyl-tRNAs from A-site to P-site by inhibiting the binding of elongation factor G to the ribosome. Spectinomycin interacts specifically with the residues G1064 and 01192 in 16S rRNA and potentially makes it inactive.Spectinomycin exhibits splicing inhibition and dependent on pH changes and Mg2+ concentration, indicating electrostatic interactions with the intron RNA.
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