Spectinomycin-dihydrochloride-pentahydrate-Spectinomycin-hydrochloride-hydrate-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESpectinomycin dihydrochloride pentahydrateCat. No.: HY-B1828ACAS No.: 22189-32-8Synonyms: Spectinomycin hydrochloride hydrate分式: CHClNO分量: 495.35作靶點(diǎn): Bacterial作通路: Anti-infection儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C

2、6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) H2O : 6.6 mg/mL (13.32 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.0188 mL 10.0939 mL 20.1877 mL5 mM 0.4038 mL 2.0188 mL 4.0375 mL10 mM 0.2019 mL 1.0094 mL 2.0188 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，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICA

3、L ACTIVITY物活性 Spectinomycin dihydrochloride pentahydrate譜的氨 環(huán)糊精抗素，可以抑制多種蘭陽性和蘭 性物的長(zhǎng)。體外研究Spectinomycin selectively inhibits protein synthesis in cells and in extracts of Escherichia coli. When addedto an exponentially growing culture, spectinomycin (50 g/mL) rapidly and reversibly inhibits growth of1/

4、2 Master of Small Molecules 您邊的抑制劑師www.MedChemEEscherichia coli. Amino acid incorporation is slowed immediately but RNA synthesis continued. In extracts ofEscherichia coli B, spectinomycin inhibits polypeptide synthesis directed either by endogenous messengerRNA or by MS-2 bacteriophage RNA. Maximum

5、 inhibition (70 to 80%) is achieved at 1 g/mL (3 M). 1.Spectinomycin blocks the translocation of peptidyl-tRNAs from the A-site to the P-site by inhibiting thebinding of elongation factor G to the ribosome. Spectinomycin interacts specifically with the residues G1064and 01192 in 16S rRNA and potenti

6、ally change this molecule into an inactive conformation 2.Spectinomycin acts as a mixed noncompetitive inhibitor for the td intron RNA with a Ki of 7.2 mM. Thesplicing inhibition by spectinomycin is dependent on pH changes and Mg2+ concentration, indicatingelectrostatic interactions with the intron

7、RNA 3.體內(nèi)研究 Renal excretion is a major elimination pathway for spectinomycin. Following IV administration, approximately55% of the drug is excreted into the urine in unchanged form. After IV administration of 10 mg/kgspectinomycin shows a peak plasma concentration of 37.8 g/mL and a systemic exposure

8、 (area-under thecurve AUC0-) of 15.7 g/mL. Following single dose intramuscular administration, the overall eliminationhalf-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 inhumans 4.PROTOCOLAnimal Rats: Spectinomycin (10 mg/kg) is administered in

9、travenously to rats. Serial blood samples (approx. 250 L)Administration 4 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 4C) and stored at 80C untilanalysis.

10、Urine samples are collected at an interval of 0-6, 6-12, 12-24, 24-36 and 36-48 h post-dose andstored at 80C until analysis 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Davies J, et al. Inhibition of protein synthesis by spectinomycin.

11、 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 thismolecule 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 Mar16;269(2):574-9.4. Madhura DB, et al. Pharmacokinetic profile of spectinomycin in rats. Pharmazie. 2013 Aug;68(8):675-6.McePdfHeightCaution: Produc