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。
生物活性 | Spectinomycin dihydrochloride is a broad-spectrumantibioticand inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin dihydrochloride acts by selectively targeting to thebacterialribosome and interrupting protein synthesis. Spectinomycin dihydrochloride is also a noncompetitive inhibitor of td intron RNA with anKivalue of 7.2 mM[1]-[5]. |
IC50& Target | bacterial ribosomal subunit[5] |
体外研究 (In Vitro) | Spectinomycin dihydrochloride selectively inhibits protein synthesis in cells and in extracts ofEscherichia coli: Spectinomycin dihydrochloride (50 μg/mL) inhibitsEscherichia coligrowth rapidly and reversibly, and suppresses amino acid incorporation immediately[1]. 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 ofEscherichia coli[1][1]. 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[2]. Spectinomycin dihydrochloride interacts specifically with the residues G1064 and 01192 in 16S rRNA and potentially makes it inactive[2]. Spectinomycin dihydrochloride exhibits splicing inhibition and dependent on pH changes and Mg2+concentration, indicating electrostatic interactions with the intron RNA[3].
|
体内研究 (In Vivo) | Spectinomycin dihydrochloride (20 mg/kg; i.m.; 20-100 mg/kg; 9 d) shows the safety in healthy chicks[4]. 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[5]. Pharmacokinetics of Spectinomycin dihydrochloride in Rat[5]
Parameter | C0(μg/mL) | AUC0-∞(μgoh/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 | / | / |
Animal Model: | Arbor Acres plus broiler chicks (15-day-old)[4] | 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. |
|
分子量 | |
性状 | |
Formula | |
CAS 号 | |
中文名称 | |
结构分类 | - Antibiotics
- Other Antibiotics
|
来源 | bacterium Streptomyces spectabilis |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: H2O : ≥ 100 mg/mL(246.75 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 2.4675 mL | 12.3375 mL | 24.6749 mL | 5 mM | 0.4935 mL | 2.4675 mL | 4.9350 mL | 10 mM | 0.2467 mL | 1.2337 mL | 2.4675 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: PBS Solubility: 50 mg/mL (123.37 mM); Clear solution; Need ultrasonic
*以上所有助溶剂都可在本网站选购。 |