盐酸大观霉素|21736-83-4|(盐酸大观霉素)-陌孚医药/Medlife

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盐酸大观霉素 (Synonyms: 盐酸大观霉素)

目录号: PC11732 纯度: ≥98%

CAS No. :21736-83-4

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中文名称	盐酸大观霉素
中文别名	盐酸大观霉素;淋必治;奇放素菌素盐酸盐;壮观霉素二盐酸盐;壮观霉素,奇霉素,奇放线菌素;大观霉素(壮观霉素);盐酸奇霉素;大观霉素;氯（五甲基环戊二烯基）{5-氰基-2-{1-[（4-甲氧基苯基）亚氨基-kN]乙基}苯基-KC}合铱（III）;壮观霉素;壮观霉素二盐酸盐五水水合物(大观霉素,奇霉素) 标准品;壮观霉素盐酸盐
英文名称	Spectinomycin dihydrochloride
英文别名	Spectinomycin Hydrochloride;M 141;stanilo;U-18409AE;NSC 248616;SPECTINOMYCIN 2HCL;Spectinomycin2HClpentahydrate;SPECTINOMYCIN DIHYDROCHLORIDE;ACTINOSPECTACIN DIHYDROCHLORIDE;SPECTINOMYCIN READY MADE SOLUTION;Spectinomycin (dihydrochloride);Spectinomycin Dihydr;Spectinomycin HCl;Spectinomycin Sulphate;spectinomycin standard solution;actinospectacin;Spectinomycin dihydrochloride pentahydrate;Spectinomycin hydrochloride anhydrous;DSSTox_CID_25429;DSSTox_RID_80873;DSSTox_GSID_45429;Spectinomycin hydrochloride hydrate;(2R,4aR,5aR,6S,7S,8R,9S,9aR,10aS)-4a,7,9-trihydroxy-2-methyl-6,8-bis(methylamino)decahydro-4H-benzo[b]pyrano[2,3-e][1,4]dioxin-
Cas No.	21736-83-4
分子式	C₁₄H₂₆Cl₂N₂O₇
分子量	405.27
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Spectinomycin dihydrochloride is a broad-spectrum antibiotic and inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin dihydrochloride acts by selectively targeting to the bacterial ribosome and interrupting protein synthesis. Spectinomycin dihydrochloride is also a noncompetitive inhibitor of td intron RNA with an K_i value of 7.2 mM.

性状

Solid

IC50 & Target[1][2]

bacterial ribosomal subunit

体外研究(In Vitro)

Spectinomycin dihydrochloride selectively inhibits protein synthesis in cells and in extracts of Escherichia coli:
Spectinomycin dihydrochloride (50 μg/mL) inhibits Escherichia coli growth rapidly and reversibly, and suppresses amino acid incorporation immediately.
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 of Escherichia coli.
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.
Spectinomycin dihydrochloride interacts specifically with the residues G1064 and 01192 in 16S rRNA and potentially makes it inactive.
Spectinomycin dihydrochloride exhibits splicing inhibition and dependent on pH changes and Mg concentration, indicating electrostatic interactions with the intron RNA.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.
Pharmacokinetics of Spectinomycin dihydrochloride in Rat

Parameter	C₀ (μg/mL)	AUC_0-∞ (μg?h/mL)	V_d (L/kg)	CL (L/h/kg)	MRT (h)	T_1/2α (h)	T_1/2β (h)	T_1/2γ (h)	f_e	CL_renal (L/h/kg)	E_ratio
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	/	/

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

运输条件

Room temperature or refrigerated transportation.

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)

结构分类

来源

bacterium Streptomyces spectabilis

参考文献

[1]. Davies J, et al. Inhibition of protein synthesis by spectinomycin. Science. 1965 Sep 3;149(3688):1096-8. [Information]

[2]. Brink MF, et al. Spectinomycin interacts specifically with the residues G1064 and C1192 in 16S rRNA, thereby potentially freezing this molecule into an inactive conformation. Nucleic Acids Res. 1994 Feb 11;22(3):325-31. [Information]

[3]. Park IK, et al. Spectinomycin inhibits the self-splicing of the group 1 intron RNA. Biochem Biophys Res Commun. 2000 Mar 16;269(2):574-9. [Information]

[4]. Khan EA, et al. Safety evaluation study of lincomycin and spectinomycin hydrochloride intramuscular injection in chickens. Toxicol Rep. 2022 Jan 29;9:204-209. [Information]

[5]. Madhura DB, et al. Pharmacokinetic profile of spectinomycin in rats. Pharmazie. 2013 Aug;68(8):675-6. [Information]

溶解度数据

体外研究:

H₂O : ≥ 100 mg/mL (246.75 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： PBS
Solubility: 50 mg/mL (123.37 mM); Clear solution; Need ultrasonic

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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