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Quinupristin-Dalfopristin Complex (mesylate)

 
Catalog No.
C5428
两种链霉素抗生素的混合物
组合的产品项目
规格价格库存 数量
5mg
¥ 3,250.00
Ship with 10-15 days
25mg
¥ 10,562.00
Ship with 10-15 days

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A

背景

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.

化学属性

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[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]([
运输条件 蓝冰运输或根据您的需求运输。
一般建议不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

试验操作

细胞实验 [1]:

细胞系

大肠杆菌ATCC 29417(MRE 600),粪肠球菌ATCC 29212,金黄色葡萄球菌ATCC 29213,流感嗜血杆菌ATCC 49247和肺炎链球菌ATCC 49619。

溶解方法

在DMSO中是可溶的。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

1 μg/ml~64 μg/ml

应用

在所有其他测试菌株中,flopristin表现出高于dalfopristin的活性,linopristin的活性与quinupristin相同或更低。对于所有菌株,dalfopristin预水解形式给药的MIC值是virginiamycin M的2倍,后者在化学上与dalfopristin的水解产物相同。

动物实验 [2]:

动物模型

葡萄球菌感染的雄性Wistar大鼠

剂量

50 mg/l quinupristin/dalfopristin浸泡

应用

Quinupristin/dalfopristin疗效显着高于左氧氟沙星和强力霉素,即使是显示细菌生长仅接受quinupristin/dalfopristin浸泡的大鼠定量移植培养物。否则,左氧氟沙星的功效与强力霉素相似。 只有用quinupristin/dalfopristin联合左氧氟沙星或强力霉素治疗的组没有葡萄球菌感染。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

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.

质量控制

质量控制和MSDS

批次:

化学结构

Quinupristin-Dalfopristin Complex (mesylate)