Posizolid
Posizolid (AZD2563), an oxazolidinone antibiotic, is developed by AstraZeneca for the study of bacterial infections. Posizolid shows very good anti-mycobacterial activity.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 252260-02-9
- 分子式: C21H21F2N3O7
- 分子量:465.40
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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Oxazolidinone |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero | IC50 |
>64 μg/mL
Compound: AZD5847
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Cytotoxicity against African green monkey Vero cells assessed as growth inhibition after 48 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as growth inhibition after 48 hrs by MTT assay
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[PMID: 28523106] |
Posizolid is determined the activity of against 250 highly resistant pneumococci and 267 drug-susceptible isolates. Posizolid MICs for 50 and 90% of the strains tested are 1 and 2 μg/ml and 0.5 and 1 μg/ml, respectively, for the two isolate groups[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In PK analysis, AZD5847(5 mg/kg) shows a low clearance (4.7 ml/min/kg) and volume of distribution (0.5 liter/kg) in mice, the half-life is 1.3 h[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c mice, aged 6 to 8 weeks, 30 to 40 g[3].
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Dosage:3, 10, 30, 100, 300, 600, and 900 mg/kg
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Administration:oral; collect blood samples at 5 min, 10 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, and 24 h
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Result:AZD5847 DSP can’t be detected in plasma 5 min.
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Animal Model:Male BALB/c mice, aged 6 to 8 weeks, 30 to 40 g[3].
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Dosage:250 mg/kg
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Administration:oral; collect blood and BAL fluid samples at 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, 16 h, 24 h, and 48 h
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Result:AZD5847(5 mg/kg) shows a low clearance (4.7 ml/min/kg) and volume of distribution (0.5 liter/kg) in mice, the half-life is 1.3 h.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 252260-02-9
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分子量 465.40
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分子式 C21H21F2N3O7
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SMILES
O=C1O[C@@H](COC2=NOC=C2)CN1C3=CC(F)=C(C4=CCN(C([C@@H](O)CO)=O)CC4)C(F)=C3
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別名
AZD2563; AZD5847
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Kumar D, et al. The anti-tuberculosis agents under development and the challenges ahead. Future Med Chem. 2015;7(15):1981-2003. [Content Brief]
[2]. Baum SE, et al. Comparative activities of the oxazolidinone AZD2563 and linezolid against selected recent North American isolates of Streptococcus pneumoniae. Antimicrob Agents Chemother. 2002;46(9):3094-3095. [Content Brief]
[3]. Balasubramanian V, et al. Pharmacokinetic and pharmacodynamic evaluation of AZD5847 in a mouse model of tuberculosis. Antimicrob Agents Chemother. 2014;58(7):4185-4190. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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