Posizolid (Synonyms: AZD2563; AZD5847)

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Posizolid (AZD2563), an oxazolidinone antibiotic, is developed by AstraZeneca for the study of bacterial infections. Posizolid shows very good anti-mycobacterial activity.

For research use only. We do not sell to patients.

Posizolid Chemical Structure

CAS No. : 252260-02-9

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Description

Posizolid (AZD2563), an oxazolidinone antibiotic, is developed by AstraZeneca for the study of bacterial infections. Posizolid shows very good anti-mycobacterial activity^[1].

IC₅₀ & Target

Oxazolidinone

Cellular Effect

Cell Line	Type	Value	Description	References
Vero	IC₅₀	> 64 μg/mL Compound: AZD5847	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	[PMID: 28523106]

In Vitro

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 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Molecular Weight

465.40

Formula

C₂₁H₂₁F₂N₃O₇

CAS No.

252260-02-9

SMILES

O=C1O[C@@H](COC2=NOC=C2)CN1C3=CC(F)=C(C4=CCN(C([C@@H](O)CO)=O)CC4)C(F)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

Posizolid Related Classifications

Infection

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Posizolid252260-02-9AZD2563 AZD5847AZD 2563AZD-2563AZD5847AZD 5847AZD-5847AntibioticoxazolidinoneantibioticAstraZenecabacterial infectionsanti-mycobacterial activityInhibitorinhibitorinhibit

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