Tedizolid
(Synonyms: 特地唑胺; TR 700; Torezolid; DA-7157) 目录号 : GC13891
An oxazolidinone antibiotic
Cas No.:856866-72-3
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
PRSP (penicillin G MICs≥2 μg/ml) clinical isolates |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
20h; MIC90=0.25 μM |
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Applications |
Agar dilution experiments demonstrated that all 28 clinical isolates of PRSP were inhibited by tedizolid at 0.25 μg/ml (MIC range, 0.125 to 0.25 μg/ml) and all were inhibited by linezolid at 1μg/ml (MIC range, 0.125 to 1 μg/ml). Tedizolid was 4-fold more potent than linezolid against PRSP; MIC90s were 0.25 μg/ml with tedizolid and 1 μg/ml with linezolid. |
| Animal experiment [1]: | |
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Animal models |
Male ICR mice |
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Dosage form |
10 mg/kg (QD); intraperitoneal inoculation |
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Applications |
The majority (80%) of the untreated control mice infected with PSSP type III succumbed to the infection within 7 days. For infected mice receiving 48 h treatment with tedizolid phosphate at 2.5 mg/kg QD and 5 mg/kg QD (total daily doses, 2.5 mg/kg and 5 mg/kg, respectively), the 15-day cumulative survival rates were 50% and 80%, respectively. A 100% survival rate was achieved with tedizolid phosphate at a minimum total daily dose of 10 mg/kg (QD), which was 4-fold lower than the 40-mg/kg total daily dose of linezolid (BID) needed to obtain 100% survival. On the basis of the ED50 values in the murine pneumococcal pneumonia model, tedizolid phosphate was nearly 3-fold more potent than linezolid, with ED50s of 2.80 mg/kg/day (95% CI, 1.41 to 4.44) versus 8.09 mg/kg/day (95% CI, 4.74 to 11.91) |
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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. |
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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. |
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| Cas No. | 856866-72-3 | SDF | |
| 别名 | 特地唑胺; TR 700; Torezolid; DA-7157 | ||
| 化学名 | (5R)-3-[3-fluoro-4-[6-(2-methyltetrazol-5-yl)pyridin-3-yl]phenyl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one | ||
| Canonical SMILES | CN1N=C(N=N1)C2=NC=C(C=C2)C3=C(C=C(C=C3)N4CC(OC4=O)CO)F | ||
| 分子式 | C17H15FN6O3 | 分子量 | 370.34 |
| 溶解度 | ≥ 9.25 mg/mL in DMSO with gentle warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7002 mL | 13.5011 mL | 27.0022 mL |
| 5 mM | 0.54 mL | 2.7002 mL | 5.4004 mL |
| 10 mM | 0.27 mL | 1.3501 mL | 2.7002 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet