Quinupristin (mesylate) (Synonyms: RP 57669,Streptogramin B) |
| Catalog No.GC17579 |
La quinupristine (mésylate) est un antibiotique streptogramine.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 120138-50-3
Sample solution is provided at 25 µL, 10mM.
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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:
[1] Allington D R, Rivey M R Quinupristid/Dalfopristin: A Therapeutic Review. Clinical Therapeutics .200 1, 23,(1): 24-44.
[2] Batard E, Jacqueline C, Boutoille D, Hamel A, Drugeon HB, Asseray N, Leclercq R, Caillon J, Potel G, Bugnon D. Combination of quinupristin-dalfopristin and gentamicin against methicillin-resistant Staphylococcus aureus: experimental rabbit endocarditis study. Antimicrob Agents Chemother. 2002 Jul;46(7):2174-8.
[3] https://en. wikipedia.org/wiki/Dalfopristin
| Cas No. | 120138-50-3 | SDF | |
| Synonymes | RP 57669,Streptogramin B | ||
| Chemical Name | 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 | ||
| Formula | C53H68N9O10S • CH3SO3 | M.Wt | 1118.3 |
| Solubility | DMSO : 125 mg/mL (122.28 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 0.8942 mL | 4.4711 mL | 8.9421 mL |
| 5 mM | 0.1788 mL | 0.8942 mL | 1.7884 mL |
| 10 mM | 0.0894 mL | 0.4471 mL | 0.8942 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)
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