Posizolid
Posizolid (AZD2563), an oxazolidinone antibiotic, is developed by AstraZeneca for the study of bacterial infections. Posizolid shows very good anti-mycobacterial activity.
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- CAS No.: 252260-02-9
- Formule: C21H21F2N3O7
- Masse moléculaire:465.40
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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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 |
Chemical Information
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CAS No. 252260-02-9
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Masse moléculaire 465.40
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Formule 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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Synonyms
AZD2563; AZD5847
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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