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Quinupristin-Dalfopristin Complex (mesylate)

Catalog No.
C5428
mixture of two streptrogramin antibiotics
Grouped product items
SizePriceStock Qty
5mg
$222.00
Ship with 5-10 days
25mg
$936.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Quinupristin-Dalfopristin Complex is a mixture of two streptrogramin antibiotics.

Quinupristin-dalfopristin complex is a mixture of two streptrogramin antibiotics, dalfopristin and quinupristin. Streptogramin antibiotics are divided into types A and B, which in combination can act synergistically.

In vitro: A previous study compared the molecular interactions of the streptogramin combinations Synercid (type A, dalfopristin; type B, quinupristin) and NXL 103 (type A, flopristin; type B, linopristin) with the Escherichia coli 70S ribosome. Results showed that the streptogramin A and B components in Synercid and NXL 103 exhibited synergistic antimicrobial activity against certain pathogenic bacteria. Moreover, in transcription-coupled translation assays, only combinations including dalfopristin, the streptogramin A component of Synercid, showed synergy [1].

In vivo: A previous animal study aimed to investigate the efficacy of quinupristin/dalfopristin in the prevention of prosthetic graft infection in a rat subcutaneous pouch model. Results showd that quinupristin/dalfopristin had a significantly higher efficacy than levofloxacin and doxycycline. In addition, only the group treated with quinupristin/dalfopristin combined with levofloxacin or doxycycline showed no evidence of staphylococcal infection [2].

Clinical trial: In a randomized multicentric trial comparing Synercid with vancomycin for the treatment of nosocomial pneumonia due to gram-positive cocci, the cure rate (56.3% vs 58.3%) were equivalent in the 2 treatment arms. Treatment failures were also similar: 44% vs 42%. Mortality (25% vs 22%) was likewise comparable, as was tolerance [3].

References:
[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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt1905.3
FormulaC34H51N4O9S[CH3SO3]·C53H68N9O10S[CH3SO3]
SynonymsRP 59500
SolubilitySoluble in ethanol;methanol;DMSO;dimethyl formamide
Chemical Name4-[4-(dimethylamino)-N-methyl-L-phenylalanine]-5-[(2S)-5-[(1-azabicyclo[2.2.2]oct-3-ylthio)methyl]-4-oxo-2-piperidinecarboxylic acid]-virginiamycin S1, monomethanesulfonate mixture with (3R,4R,5E,10E,12E,14S,26R,26aS)-26-[[2-(diethylamino)ethyl
SDFDownload SDF
Canonical SMILESO=C1C[[email protected]]([H])(N(C[[email protected]]1CS[[email protected]@H]2C[NH+]3CCC2CC3)C([[email protected]@]([H])(N(C([[email protected]@]4(CCCN4C([[email protected]@H](CC)N5)=O)[H])=O)C)CC6=CC=C(C=C6)N(C)C)=O)C(N[[email protected]](C(O[[email protected]@H]([[email protected]@H](C5=O)NC(C7=C(C=CC=N7)O)=O)C)=O)C8=CC=CC=C8)=O.CS([O-])(=O)=O.O=C(NC/C=C\C(C)=C\[[email protected]](C9)O)/C=C/[[email protected]]([
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

Cell experiment [1]:

Cell lines

E.coli ATCC 29417 (MRE 600), Enterococcus faecalis ATCC 29212, S.aureus ATCC 29213, Haemophilus influenzae ATCC 49247, and Streptococcus pneumoniae ATCC 49619.

Preparation method

The solubility of this compound in DMSO is soluble. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1 μg/ml~64 μg/ml

Applications

In all other tested strains, flopristin exhibited higher activity than dalfopristin, and linopristin had the same or lower activity as quinupristin. For all strains, the MIC value of the dalfopristin pre-hydrolyzed form was twice that of virginin M, which was chemically the same as the hydrolysate of dalfopristin.

Animal experiment [1]:

Animal models

Staphylococcus-infected male Wistar rats

Dosage form

50 mg/l quinupristin/dalfopristin-soaked

Application

Quinupristin / dalfopristin was significantly more effective than levofloxacin and doxycycline, even if it showed bacterial growth in rats receiving only quinupristin / dalfopristin soaked in quantitative transplant cultures. Otherwise, the efficacy of levofloxacin is similar to doxycycline. Only groups treated with quinupristin / dalfopristin in combination with levofloxacin or doxycycline had no staphylococcal infection.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Noeske J, Huang J, Olivier NB, Giacobbe RA, Zambrowski M, Cate JH. Synergy of streptogramin antibiotics occurs independently of their effects on translation. Antimicrob Agents Chemother. 2014 Sep;58(9):5269-79. doi: 10.1128/AAC.03389-14.Epub 2014 Jun 23. PubMed PMID: 24957822; PubMed Central PMCID: PMC4135883.

[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. PubMed PMID:12217284.

Quality Control

Quality Control & MSDS

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Chemical structure

Quinupristin-Dalfopristin Complex (mesylate)