Tedizolid HCl
目录号 : GC15288
Oxazolidinone for gram-positive infections
Sample solution is provided at 25 µL, 10mM.
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IC50: for MAO-A (monoamine oxidase-A), 8.7 uM; for MAO-B, 5.7 uM.
Tedizolid HCl is a reversible, novel oxazolidinone antibiotic. It is the first oxazolidinone to be approved since linezolid in 2000. Tedizolid phosphate is the second commercially available oxazolidinone antibiotic and is the prodrug form of tedizolid with a fixed once-daily dose. As an expanded-spectrum oxazolidinone it has potent activity against a wide range of Gram-positive pathogens [1].
In vitro: In vitro, tedizolid was a reversible inhibitor for both human MAO-A and MAO-B; for MAO-A, the value of IC50 was 8.7 uM, and for MAO-B, the value of IC50 was 5.7 uM. For this two inhibitions, add 46.0 and 2.1 uM of linezolid, respectively would be better [2].
In vivo: It exhibited not only a potent activity against Gram-positive pathogens but also maintained activity against linezolid resistant bacteria. In murine serotonergic model, the number of head twitches was analyzed after tedizolid phosphate was administrated by intraperitoneal injection [2].
Clinical trial: With 200 mg once daily tedizolid would treat the acute bacterial skin and skin structure infections caused by gram-positive bacteria in phase III clinical trials. The treatment effects of tedizolid for ventilator-acquired and health care-associated pneumonia were currently investigated [3].
References:
[1] Chen KH, Huang YT, Liao CH et dl. In Vitro Activities of Tedizolid and Linezolid against Gram-Positive Cocci Associated with Acute Bacterial Skin and Skin Structure Infections and Pneumonia. Antimicrob Agents Chemother. 2015 Oct;59(10):6262-5.
[2] S. Flanagan, K. Bartizal, S. L. Minassian et dl. In Vitro, In Vivo, and Clinical Studies of Tedizolid To Assess the Potential for Peripheral or Central Monoamine Oxidase Interactions. Antimicrob Agents Chemother. 2013 Jul;57(7):3060-6.
[3] Rybak JM, Marx K, Martin CA. Early experience with tedizolid: clinical efficacy, pharmacodynamics, and resistance. Pharmacotherapy. 2014 Nov;34(11):1198-208.
| Cas No. | N/A | SDF | |
| 化学名 | (R)-3-(3-fluoro-4-(6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one hydrochloride | ||
| Canonical SMILES | FC1=CC(N2C[C@H](CO)OC2=O)=CC=C1C3=CC=C(C4=NN(C)N=N4)N=C3.Cl | ||
| 分子式 | C17H16ClFN6O3 | 分子量 | 406.80 |
| 溶解度 | ≥ 13.57mg/mL in DMSO with gentle warming, Limited solubility in EtOH | 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 | 2.4582 mL | 12.2911 mL | 24.5821 mL |
| 5 mM | 0.4916 mL | 2.4582 mL | 4.9164 mL |
| 10 mM | 0.2458 mL | 1.2291 mL | 2.4582 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