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Spectinomycin (hydrochloride hydrate) Sale

(Synonyms: 奇霉素;大观霉素;盐酸大观霉素五水合物; Spectinomycin hydrochloride hydrate) 目录号 : GC13981

Spectinomycin是一种广谱类抗生素,可抑制多种革兰氏阳性菌和革兰氏阴性菌的生长

Spectinomycin (hydrochloride hydrate) Chemical Structure

Cas No.:22189-32-8

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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Animal experiment:

Rats: Spectinomycin (10 mg/kg) is administered intravenously to rats. Serial blood samples (approx. 250 μL) are collected pre-dose, and at 0.25, 0.5, 0.75, 1.0, 1.5, 2.0, 4.0, 6.0, 8.0, 12.0, 24.0, 36.0 and 48.0 h post-dose. Plasma is separated immediately by centrifugation (10,000g for 5 min at 4°C) and stored at −80°C until analysis. Urine samples are collected at an interval of 0-6, 6-12, 12-24, 24-36 and 36-48 h post-dose and stored at −80°C until analysis[4].

References:

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

产品描述

Spectinomycin is a broad-spectrum antibiotic that inhibits the growth of a variety of Gram-positive and Gram-negative bacteria. Spectinomycin is also a non-competitive inhibitor of TD intron RNA with a Ki value of 7.2 mM [1].

Spectinomycin is an aminocyclic alcohol antibiotic produced by S. spectabilis. It inhibits microbial protein synthesis by binding to the 30S ribosomal subunit and protects the N-7 position of G1064 nucleotide on E. coli 16S rRNA from dimethyl sulfate. base. Spectinomycin binds to this position and is thought to stabilize helix 34, thereby inhibiting the binding of elongation factor G, preventing the transfer of peptide-tRNA from the A site to the P site of the ribosome, thereby inhibiting protein synthesis [2]. Mutations in the ribosomal protein S5 gene can prevent the binding of Spectinomycin and contribute to bacterial resistance [3].

In cell culture experiments, the recommended concentration of Spectinomycin is 7.5-20 μg/mL.

 

Spectinomycin是一种广谱类抗生素,可抑制多种革兰氏阳性菌和革兰氏阴性菌的生长。Spectinomycin也是TD内含子RNA的非竞争性抑制剂,Ki值为7.2 mM[1]

Spectinomycin是由S. spectabilis产生的氨基环醇类抗生素,通过与30S核糖体亚基结合抑制微生物蛋白质合成,并保护大肠杆菌16S rRNAG1064核苷酸的N-7位置不被二甲基硫酸甲基化。Spectinomycin结合于该位置,被认为稳定了34号螺旋,从而抑制了伸长因子G的结合,阻止了肽-tRNA从核糖体A位点转移到P位点,从而抑制蛋白合成[2]。核糖体蛋白S5基因的突变能够阻止Spectinomycin的结合,有助于细菌的耐药性[3]

在细胞培养实验中,Spectinomycin的建议浓度为7.5-20μg/mL

 

References:

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

[2] Zimmerman J M, Maher L J.  In vivo selection of spectinomycin‐binding RNAs[J]. Nucleic acids research, 2002, 30(24): 5425-5435.

[3] Kehrenberg, C., and Schwarz, S. Mutations in 16S rRNA and ribosomal protein S5 associated with high-level spectinomycin resistance in Pasteurella multocida. Antimicrob. Agents Chemother. 51(6), 2244-2246 (2007).

Chemical Properties

Cas No. 22189-32-8 SDF
别名 奇霉素;大观霉素;盐酸大观霉素五水合物; Spectinomycin hydrochloride hydrate
化学名 (5aR,9aR,10aS)-decahydro-4aR,7S,9S-trihydroxy-2R-methyl-6S,8R-bis(methylamino)-4H-pyrano[3-b][1,4]benzodioxin-4-one, dihydrochloride pentahydrate
Canonical SMILES [H][C@@]12[C@@](C(C[C@@H](C)O2)=O)(O)O[C@]3([H])[C@@H](NC)[C@@H](O)[C@@H](NC)[C@H](O)[C@@]3([H])O1.Cl.Cl.O.O.O.O.O
分子式 C14H24N2O7 • 2HCl [5H2O] 分子量 495.4
溶解度 ≥ 49.5mg/mL in H20, ≥ 92 mg/mL in DMSO, ≥ 3.61 mg/mL in EtOH with ultrasonic and warming 储存条件 Store at 2-8°C,argon filling away from moisture
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1 mM 2.0186 mL 10.0929 mL 20.1857 mL
5 mM 0.4037 mL 2.0186 mL 4.0371 mL
10 mM 0.2019 mL 1.0093 mL 2.0186 mL
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