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Quinupristin (mesylate) (120138-50-3 free base)

Catalog No. TP2286 CAS TP2286

Synonyms: Quinupristin (mesylate)

Quinupristin is a streptogramin antibiotic. Streptogramins, a class of antibiotics, is 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.

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Quinupristin (mesylate) (120138-50-3 free base) Chemical Structure

Quinupristin (mesylate) (120138-50-3 free base), CAS TP2286

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Quinupristin is a streptogramin antibiotic. Streptogramins, a class of antibiotics, is 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	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	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 logs CFU/g (control group) to 3.0 ± 0.9 (Q-D) and 2.6 ± 0.5 logs 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 logs CFU/g (control group) 5.2 ± 2.2 (Q-D) 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].

Synonyms	Quinupristin (mesylate)
Molecular Weight	1118.3
Formula	C53H68N9O10S·CH3SO3
CAS No.	TP2286

Storage

keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: Soluble

Ethanol: Soluble

References and Literature

1. Noeske, J. ,Huang, J.,Olivier, N.B., et al. Synergy of streptogramin antibiotics occurs independently of their effects on translation. Antimicrobial Agents and Chemotherapy 58(9), 5269-5279 (2014). 2. Ghiselli R, Giacometti A, Cirioni O, Mocchegiani F, Orlando F, Del Prete M, D'Amato G, Scalise G, Saba V. Quinupristin/dalfopristin bonding in combination with intraperitoneal antibiotics prevent infection of knitted polyester graft material in a subcutaneous rat pouch model infected with resistant Staphylococcus epidermidis. Eur J Vasc Endovasc Surg. 2002 Sep;24(3):230-4. 3. Potel G. Value of Synercid in clinical practice: from temporary approval to clinical trial authorization. Presse Med. 2001 Sep 8;30(25 Pt 2):XIX-XXII.

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Keywords

Quinupristin (mesylate) (120138-50-3 free base) TP2286 Others Quinupristin (mesylate) (120138503 free base) Quinupristin (mesylate) (120138 50 3 free base) 120138-50-3 Quinupristin (mesylate) 120138-50-3 free base Quinupristin inhibitor inhibit

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