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Quinupristin-Dalfopristin Complex (mesylate) Sale

(Synonyms: RP 59500) 目录号 : GC11466

A mixture of streptogramin antibiotics

Quinupristin-Dalfopristin Complex (mesylate) Chemical Structure

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5mg
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25mg
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产品描述

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

Cas No. SDF
别名 RP 59500
化学名 4-[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
Canonical SMILES O=C1C[C@]([H])(N(C[C@H]1CS[C@@H]2C[NH+]3CCC2CC3)C([C@@]([H])(N(C([C@@]4(CCCN4C([C@@H](CC)N5)=O)[H])=O)C)CC6=CC=C(C=C6)N(C)C)=O)C(N[C@H](C(O[C@@H]([C@@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\[C@H](C9)O)/C=C/[C@H]([
分子式 C34H51N4O9S[CH3SO3] • C53H68N9O10S[CH3SO3] 分子量 1905.3
溶解度 Soluble in ethanol;methanol;DMSO;dimethyl formamide 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 0.5249 mL 2.6243 mL 5.2485 mL
5 mM 0.105 mL 0.5249 mL 1.0497 mL
10 mM 0.0525 mL 0.2624 mL 0.5249 mL
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