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].
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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. |
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| 结构分类 | - Antibiotics
- Other Antibiotics
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| 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。 |
