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22189-32-8

中文名稱 鹽酸大觀霉素五水合物
英文名稱 Spectinomycin dihydrochloride pentahydrate
CAS 22189-32-8
分子式 C14H24N2O7.2HCl.5H2O
分子量 495.35
MOL 文件 22189-32-8.mol
更新日期 2025/01/07 14:34:22
22189-32-8 結(jié)構(gòu)式 22189-32-8 結(jié)構(gòu)式

基本信息

中文別名
鹽酸奇霉素
壯觀霉素鹽酸鹽
壯觀霉素1GM
奇放線霉素鹽酸鹽
壯觀霉素(標(biāo)準(zhǔn)品)
鹽酸大觀霉素,五水
鹽酸壯觀霉素五水合物
壯觀霉素鹽酸鹽水合物
大觀霉素鹽酸鹽水合物
鹽酸大觀霉素五水合物
英文別名
M 141
D00869
U-18409AE
spectogard
Trobicin (tn)
SPECTINOMYCIN HCL
SPECTINOMYCIN 2HCL
Spectinomycin,≥98%
Spectinomycin HCL USP/BP
Spectinomycin dihydrochL
所屬類別
原料藥:抗真菌類藥

物理化學(xué)性質(zhì)

熔點(diǎn)205-207° (dec)
比旋光度D +14.8° (c = 0.42 in water)
儲(chǔ)存條件2-8°C
溶解度H2O: 50 mg/mL, clear, faintly yellow
形態(tài)powder
顏色白色至灰白色
水溶解性Soluble in water.Soluble in water, methanol, dimethyl sulfoxide, ethanol and dimethyl formamide.
Merck14,8739
BRN5684150
InChIKeyDCHJOVNPPSBWHK-UXXUFHFZSA-N
CAS 數(shù)據(jù)庫22189-32-8

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H315-H319-H335
安全說明24/25
WGK Germany2
RTECS號(hào)WG7400000
海關(guān)編碼29419090
毒性mouse,LD50,intramuscular,> 5gm/kg (5000mg/kg),BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY),Japanese Journal of Antibiotics. Vol. 29, Pg. 43, 1976.

應(yīng)用領(lǐng)域

用途1
靠干擾肽基tRNA轉(zhuǎn)錄抑制蛋白酶合成。對(duì)象為革蘭氏陰性和陽性菌。 抑制模式: rpsE (核糖體蛋白S5基因)基因的變異能阻止大觀霉素的結(jié)合。

常見問題列表

生物活性
Spectinomycin dihydrochloride pentahydrate是廣譜的氨基環(huán)糊精抗生素,可以抑制多種革蘭氏陽性和革蘭氏陰性生物的生長(zhǎng)。
體外研究

Spectinomycin selectively inhibits protein synthesis in cells and in extracts of Escherichia coli . When added to an exponentially growing culture, spectinomycin (50 μg/mL) rapidly and reversibly inhibits growth of Escherichia coli . Amino acid incorporation is slowed immediately but RNA synthesis continued. In extracts of Escherichia coli B, spectinomycin inhibits polypeptide synthesis directed either by endogenous messenger RNA or by MS-2 bacteriophage RNA. Maximum inhibition (70 to 80%) is achieved at 1 μg/mL (3 μM). . Spectinomycin blocks the translocation of peptidyl-tRNAs from the A-site to the P-site by inhibiting the binding of elongation factor G to the ribosome. Spectinomycin interacts specifically with the residues G1064 and 01192 in 16S rRNA and potentially change this molecule into an inactive conformation. Spectinomycin acts as a mixed noncompetitive inhibitor for the td intron RNA with a K i of 7.2 mM. The splicing inhibition by spectinomycin is dependent on pH changes and Mg 2+ concentration, indicating electrostatic interactions with the intron RNA.

體內(nèi)研究

Renal excretion is a major elimination pathway for spectinomycin. Following IV administration, approximately 55% of the drug is excreted into the urine in unchanged form. After IV administration of 10 mg/kg spectinomycin shows a peak plasma concentration of 37.8 μg/mL and a systemic exposure (area-under the curve AUC 0-∞ ) of 15.7 μg/mL. Following single dose intramuscular administration, the overall elimination half-life of spectinomycin is 1.2 h in cattle, 1.0 h in sheep, 1.0 h in pigs, 1.65 h in chicken and 1.85 h in humans.

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