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HY-B0438 鹽酸奇霉素

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型號(hào) HY-B0438: 訪問次數(shù)
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產(chǎn)地 浙江杭州市: 更新時(shí)間
2024/6/26 11:49:21

規(guī)格

500mg

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Spectinomycin dihydrochloride

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鹽酸奇霉素產(chǎn)品參數(shù)

CAS號(hào)	21736-83-4	產(chǎn)地	國(guó)產(chǎn)
規(guī)格	500mg	級(jí)別	化工級(jí)
證書	ISO系列證書

Spectinomycin dihydrochloride 是一種廣譜抗sheng素，可以抑制多種革蘭氏陽(yáng)性和革蘭氏陰性細(xì)菌的生長(zhǎng)。Spectinomycin dihydrochloride 通過特異靶向細(xì)菌核糖體，干擾蛋白質(zhì)合成。Spectinomycin dihydrochloride 也是 td 內(nèi)含子 RNA 的非競(jìng)爭(zhēng)性抑制劑，Ki 為 7.2 mM。

鹽酸奇霉素詳細(xì)信息

Spectinomycin dihydrochloride (Synonyms: 鹽酸奇霉素)

Spectinomycin dihydrochloride 是一種廣譜抗生sheng素，可以抑制多種革蘭氏陽(yáng)性和革蘭氏陰性細(xì)菌的生長(zhǎng)。Spectinomycin dihydrochloride 通過特異靶向細(xì)菌核糖體，干擾蛋白質(zhì)合成。Spectinomycin dihydrochloride 也是 td 內(nèi)含子 RNA 的非競(jìng)爭(zhēng)性抑制劑，K_i 為 7.2 mM。

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^[1]^-^[5].

IC₅₀ & Target

bacterial ribosomal subunit^[5]

體外研究(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^[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 of Escherichia 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].

體內(nèi)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)	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	/	/

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：405.27

Formula：C₁₄H₂₆Cl₂N₂O₇

CAS 號(hào)：21736-83-4

中文名稱：鹽酸奇霉素；鹽酸壯觀mei素

來源：bacterium Streptomyces spectabilis

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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)

溶解性數(shù)據(jù)

In Vitro:

H₂O : ≥ 100 mg/mL (246.75 mM)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液

濃度溶劑體積質(zhì)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

請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

參考文獻(xiàn)

[1]. Davies J, et al. Inhibition of protein synthesis by spectinomycin. Science. 1965 Sep 3;149(3688):1096-8.
[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.
[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.
[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.
[5]. Madhura DB, et al. Pharmacokinetic profile of spectinomycin in rats. Pharmazie. 2013 Aug;68(8):675-6.
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