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Tedizolid

现货
Catalog No.
A3863
恶唑烷酮,用于革兰氏阳性菌感染。
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,320.00
现货
5mg
¥ 1,200.00
现货
10mg
¥ 1,800.00
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50mg
¥ 5,200.00
现货

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Background

Tedizolid is an oxazolidinone antimicrobial agent with MIC50 value of 0.5 μg/ml for MSSA, MRSA, VR E. faecium and VR E. faecalis and 0.25 μg/ml for MSSE, MRSE, PSSP and PRSP [1].

The resistant Gram-positive infection is a serious global health problem. For instant, the methicillin-resistant S. aureus (MRSA) has spread all over the world with rates ranging from 18 to 26 cases among 100,000 people. Besides that, there come out a serious of resistant strains such as the linezolid-resistant S. aureus (LRSA) and the vancomycin-resistant S. aureus (VRSA). Due to the unfavorable outcomes of the existed antibiotics, alternative treatments have been developed. Tedizolid is a synthetic antibiotic that works based on the inhibition of protein synthesis. It binds to the 50S ribosome and inhibits the formation of the 70S complex [1].

Tedizolid showed potent bacteriostatic activity against many resistant Gram-positive pathogens such as MSSA, MRSA, S. pyogenes and S. pneumoniae. For the enterococcal and staphylococcal isolates, tedizolid displayed more than 4-fold higher potency than that of linezolid. It also showed inhibitory effects on a panel of 169 linezolid-resistant staphylococcal isolates with 79.2% inhibition at concentration of ≤ 4μg/ml. The MIC values of tedizolid against linezolid-resistant staphylococci were in a range from 0.06 to 16 mg/L. Besides that, tedizolid was found to be the inhibitors of human monoamine oxidase with IC50 values of 8.7 and 5.7 μM for MAO-A and MAO-B, respectively [1, 2 and 3].

When treated in vivo, tedizolid was the active moiety converted from the pro-drug tedizolid phosphate. It was found that granulocytes could affect the antistaphylococcal effect of tedizolid. In neutropenic mice, the administration of tedizolid for 24 hours or 48 hours caused ED50 values of 25.2 and 35.7 mg/kg/day, respectively [1 and 4].

References:
[1] Kanafani Z A, Corey G R.  Tedizolid (TR-701): a new oxazolidinone with enhanced potency. Expert opinion on investigational drugs, 2012, 21(4): 515-522.
[2] Rodríguez-Avial I, Culebras E, Betriu C, et al.  In vitro activity of tedizolid (TR-700) against linezolid-resistant staphylococci. Journal of antimicrobial chemotherapy, 2012, 67(1): 167-169.
[3] Flanagan S, Bartizal K, Minassian S L, et al.  In vitro, in vivo, and clinical studies of tedizolid to assess the potential for peripheral or central monoamine oxidase interactions. Antimicrobial agents and chemotherapy, 2013, 57(7): 3060-3066.
[4] Louie A, Liu W, Kulawy R, et al.  In vivo pharmacodynamics of torezolid phosphate (TR-701), a new oxazolidinone antibiotic, against methicillin-susceptible and methicillin-resistant Staphylococcus aureus strains in a mouse thigh infection model. Antimicrobial agents and chemotherapy, 2011, 55(7): 3453-3460.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt370.34
Cas No.856866-72-3
FormulaC17H15FN6O3
SynonymsTR-700; DA-7157; Torezolid; TR 700; DA 7157
Solubility≥9.25 mg/mL in DMSO with gentle warming, <2.37 mg/mL in EtOH, <2.58 mg/mL in H2O
Chemical Name(5R)-3-[3-fluoro-4-[6-(2-methyltetrazol-5-yl)pyridin-3-yl]phenyl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one
SDFDownload SDF
Canonical SMILESCN1N=C(N=N1)C2=NC=C(C=C2)C3=C(C=C(C=C3)N4CC(OC4=O)CO)F
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

试验操作

细胞实验[1]:

细胞系

PRSP临床分离物(penicillin G MIC ≥ 2 μg/ ml)

溶解方法

该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月

反应条件

20 h,MIC90 = 0.25 μM

实验结果

琼脂稀释实验表明,0.25 μg/mltedizolid抑制所得到的28个PRSP的临床分离物(MIC范围,0.125至0.25 μg/ml),1 μg/ml的linezolid将其完全抑制(MIC范围,0.125 to 1 μg/ml)。针对PRSP,Tedizolid比linezolid的效力高4倍,Tedizolid和linezolid 的MIC90分别为0.25 μg/ml和1 μg/ml

动物实验[1]:

动物模型

Male ICR小鼠

剂量

10 mg/kg (QD),腹膜内注射

实验结果

PSSP III型感染的大部分未处理的对照小鼠在7天内死于感染(80%)。使用每日总剂量为2.5 mg/kg QD和5 mg/kg QD的tedizolid phosphate治疗感染小鼠48小时,15天累积存活率分别为50%和80%。每日使用10 mg/kg(QD)的最小总剂量tedizolid达到100%存活率,每日使用40 mg/kg的linezolid (BID)才能获得100%存活率,是使用tedizolid的4倍。基于鼠肺炎球菌肺炎模型的ED50值,Tedizolid phosphate的效力比linezolid高近3倍,ED50为2.8mg/kg/天(95%CI,1.41至4.44),而linezolid的ED50为8.09 mg/kg/天(95%CI,4.74至11.91)

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] Choi S, Im W, Bartizal K. Activity of Tedizolid Phosphate (TR-701) in murine models of infection with penicillin-resistant and penicillin-sensitive streptococcus pneumoniae[J]. Antimicrobial agents and chemotherapy, 2012, 56(9): 4713-4717.

生物活性

描述 Torezolid(TR-701或tedizolid)是一种恶唑烷酮类抗生素药。
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