posizolid
posizolid Basic information
- Product Name:
- posizolid
- Synonyms:
-
- posizolid
- (5R)-3-[4-[1-[(2S)-2,3-Dihydroxy-1-oxopropyl]-1,2,3,6-tetrahydro-4-pyridinyl]-3,5-difluorophenyl]-5-[(3-isoxazolyloxy)methyl]-2-oxazolidinone
- Posizolid,(5R)-3-[4-[1-[(2S)-2,3-Dihydroxy-1-oxopropyl]-1,2,3,6-tetrahydro-4-pyridinyl]-3,5-difluorophenyl]-5-[(3-isoxazolyloxy)Methyl]-2-oxazolidinone
- (5R)-3-[4-[1-[(2S)-2,3-dihydroxypropanoyl]-3,6-dihydro-2H-pyridin-4-yl]-3,5-difluorophenyl]-5-(1,2-oxazol-3-yloxymethyl)-1,3-oxazolidin-2-one
- 2-Oxazolidinone, 3-[4-[1-[(2S)-2,3-dihydroxy-1-oxopropyl]-1,2,3,6-tetrahydro-4-pyridinyl]-3,5-difluorophenyl]-5-[(3-isoxazolyloxy)methyl]-, (5R)-
- posizoli
- posizolid ISO 9001：2015 REACH
- Posizolid-13C2D4
- CAS:
- 252260-02-9
- MF:
- C21H21F2N3O7
- MW:
- 465.407
- Mol File:
- 252260-02-9.mol
posizolid Chemical Properties
- Boiling point:
- 724.5±60.0 °C(Predicted)
- Density
- 1.491
- pka
- 12.79±0.20(Predicted)
posizolid Usage And Synthesis
Uses
Posizolid (AZD2563), an oxazolidinone antibiotic, is developed by AstraZeneca for the study of bacterial infections. Posizolid shows very good anti-mycobacterial activity[1].
in vivo
AZD5847 DSP (AZD2563 is prodrug) could not be detected in plasma 5 min after oral administration, suggesting rapid conversion of the prodrug to the parent molecule.
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].
| Animal Model: | Male BALB/c mice, aged 6 to 8 weeks, 30 to 40 g[3]. |
| Dosage: | 3, 10, 30, 100, 300, 600, and 900 mg/kg |
| 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 |
| Result: | AZD5847 DSP can’t be detected in plasma 5 min. |
| Animal Model: | Male BALB/c mice, aged 6 to 8 weeks, 30 to 40 g[3]. |
| Dosage: | 250 mg/kg |
| 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 |
| 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. |
IC 50
Oxazolidinone
References
[1] Kumar D, et al. The anti-tuberculosis agents under development and the challenges ahead. Future Med Chem. 2015;7(15):1981-2003. DOI:10.4155/fmc.15.128
[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. DOI:10.1128/AAC.46.9.3094-3095.2002
[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. DOI:10.1128/AAC.00137-14
posizolidSupplier
- Tel
- 13412890622
- Tel
- +8615255079626
- eric@witopchemical.com
- Tel
- +86-29-89586680 +86-15129568250
- 1026@dideu.com
- Tel
- +8618523575427
- sales@conier.com
- Tel
- 1173954148q
- meishipharma@126.com