| CAS NO: | 120138-50-3 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| Cas No. | 120138-50-3 |
| 别名 | 奎奴普丁 |
| 化学名 | 4-[4-(dimethylamino)-N-methyl-L-phenylalanine]-5-[(2S,5R)-5-[[[(3S)-1-azabicyclo[2.2.2]oct-3-yl]thio]methyl]-4-oxo-2-piperidinecarboxylic acid]-virginiamycin S1, monomethanesulfonate |
| Canonical SMILES | O=C1C[C@](C(N[C@@H](C2=CC=CC=C2)C(O[C@H](C)[C@H](NC(C3=C(O)C=CC=N3)=O)C4=O)=O)=O)([H])N(C([C@@](CC5=CC=C(N(C)C)C=C5)([H])N(C)C([C@]6([H])CCCN6C([C@H](N4)CC)=O)=O)=O)C[C@H]1CS[C@@H]7C[NH+]8CCC7CC8.CS([O-])(=O)=O |
| 分子式 | C53H68N9O10S o CH3SO3 |
| 分子量 | 1118.3 |
| 溶解度 | Soluble in ethanol;methanol;DMSO;dimethyl formamide |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Quinupristin is a streptogramin antibiotic. Streptogramins, a class of antibiotics, are effective in the treatment of vancomycin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus, which are two of the most rapidly growing strains of multidrug-resistant bacteria. Streptogramins fall into two groups: streptogramin A and streptogramin B. In vitro: Quinupristin can bind to sequential sites located on the 50s subunit of the bacterial ribosome. Dalfopristin binding causes a conformational change in the ribosome that subsequently increases the binding of quinupristin. The combined actions of the two agents create a stable drug-ribosome complex causing inhibition of protein synthesis by prevention of peptide-chain formation, blockade of extrusion of newly formed peptide chains, and bacterial cell death [1]. In vivo: The combination of quinupristin-dalfopristin (Q-D) and gentamicin was tested against two strains of gentamicin- and dalfopristin-susceptible methicillin-resistant Staphylococcus aureus (MRSA). A rabbit endocarditis model simulated the pharmacokinetics achieved in humans receiving intravenous injections of Q-D and gentamicin. For the MLSB-susceptible strain, a 4-day regimen reduced mean bacterial titers (MBT) in vegetations from 8.5 ± 0.8 log CFU/g (control group) to 3.0 ± 0.9 (Q-D) and 2.6 ± 0.5 log CFU/g (Q-D plus gentamicin). For the strain constitutively resistant to MLSB, a 4-day regimen reduced MBT in vegetations from 8.7 ± 0.9 log CFU/g (control group) 5.2 ± 2.2 (Q-D) and and 5.1 ± 2.4 log CFU/g (Q-D plus gentamicin). The differences between control and treatment groups were significant for both strains, although there was no significant difference between treatment groups [2]. Clinical trial: The combination quinupristin/dalfopristin (Synercid) was brought to the market by in 1999. Synercid is clinically used to treat infections by staphylococci and by vancomycin-resistant Enterococcus faecium [3]. References: |
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