Spectinomycin dihydrochloride pentahydrate,22189-32-8

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产品名称：Spectinomycin dihydrochloride pentahydrate

产品别名：盐酸大观霉素五水合物

英文别名：Spectinomycin dihydrochloride pentahydrate

靶点：Antibacterial

CAS：22189-32-8

纯度：＞98%

外观：白色或类白色结晶性粉末

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

An antibiotic produced by Streptomyces spectabilis. It is active against gram-negative bacteria and used for the treatment of gonorrhea.

溶解性：H2O : ≥ 6.6 mg/mL (13.32 mM)

体外研究：

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 Mg²⁺ concentration, indicating electrostatic interactions with the intron RNA.

体内研究：

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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