产品
编 号：F279151
分子式：C14H36Cl2N2O12
分子量：495.35
分子式：C14H36Cl2N2O12
分子量：495.35
产品类型
规格
价格
是否有货
500mg
400
In-stock
结构图
CAS No: 22189-32-8
产品详情
生物活性：
Spectinomycin dihydrochloride pentahydrate is a broad-spectrum antibiotic and inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin dihydrochloride pentahydrate acts by selectively targeting to the bacterial ribosome and interrupting protein synthesis. Spectinomycin dihydrochloride pentahydrate is also a noncompetitive inhibitor of td intron RNA with an Ki value of 7.2 mM-.
体内研究：
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 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 dihydrochloride pentahydrate selectively inhibits protein synthesis in cells and in extracts of Escherichia coli: Spectinomycin dihydrochloride pentahydrate (50 μg/mL) inhibits Escherichia coli growth rapidly and reversibly, and suppresses amino acid incorporation immediately. Spectinomycin dihydrochloride pentahydrate (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 pentahydrate 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 pentahydrate interacts specifically with the residues G1064 and 01192 in 16S rRNA and potentially makes it inactive.Spectinomycin dihydrochloride pentahydrate exhibits splicing inhibition and dependent on pH changes and Mg2+ concentration, indicating electrostatic interactions with the intron RNA.
Spectinomycin dihydrochloride pentahydrate is a broad-spectrum antibiotic and inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin dihydrochloride pentahydrate acts by selectively targeting to the bacterial ribosome and interrupting protein synthesis. Spectinomycin dihydrochloride pentahydrate is also a noncompetitive inhibitor of td intron RNA with an Ki value of 7.2 mM-.
体内研究：
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 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 dihydrochloride pentahydrate selectively inhibits protein synthesis in cells and in extracts of Escherichia coli: Spectinomycin dihydrochloride pentahydrate (50 μg/mL) inhibits Escherichia coli growth rapidly and reversibly, and suppresses amino acid incorporation immediately. Spectinomycin dihydrochloride pentahydrate (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 pentahydrate 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 pentahydrate interacts specifically with the residues G1064 and 01192 in 16S rRNA and potentially makes it inactive.Spectinomycin dihydrochloride pentahydrate exhibits splicing inhibition and dependent on pH changes and Mg2+ concentration, indicating electrostatic interactions with the intron RNA.
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