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Linezolid (PNU-100766)

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Linezolid (PNU-100766)
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5g$1400Check With Us

Cat #: V2009 CAS #: 165800-03-3 Purity ≥ 98%

Description: Linezolid (also known as PNU-100766), a synthetic oxazolidinone antimicrobial, is an antibiotic used for the treatment of serious infections. Linezolid shows a wide spectrum against Gram-positive bacteria andmultidrug-resistant bacteria such as anaerobes, methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant enterococci, penicillin-resistant pneumococci and streptococcus. Linezolid inhibits initiation complex formation with either the 30S or the 70S ribosomal subunits from Escherichia coli. Linezolid inhibits complex formation with Staphylococcus aureus 70S tight-couple ribosomes.

References: [1]. Clemett D, Markham A. Linezolid. Drugs. 2000 Apr;59(4):815-27; discussion 828.

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Molecular Weight (MW)337.35
Molecular FormulaC16H20FN3O4
CAS No.165800-03-3
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 67 mg/mL (198.6 mM)r
Water: <1 mg/mLr
Ethanol: 8 mg/mL (23.7 mM)
Solubility In Vivo30% PEG400+0.5% Tween80+5% Propylene glycol: 30 mg/mL
SMILES CodeCC(=O)NC[C@H]1CN(C(=O)O1)C2=CC(=C(C=C2)N3CCOCC3)F
SynonymsPNU 100766; PNU-100766; PNU100766; U 100766; U-100766; U100766; Linezolid; Zyvox; Zyvoxid; Zyvoxam
ProtocolIn VitroIn vitro activity: Linezolid inhibits initiation complex formation with either the 30S or the 70S ribosomal subunits from Escherichia coli. Linezolid inhibits complex formation with Staphylococcus aureus 70S tight-couple ribosomes. Linezolid is a potent inhibitor of cell-free transcription-translation in E. coli, exhibiting 50% inhibitory concentrations (IC50s) of 1.8 mM. Linezolid is an oxazolidinone, a new class of antibacterial agents with enhanced activity against pathogens. Linezolid MICs vary slightly with the test method, laboratory, and significance attributed to thin hazes of bacterial survival, but all workers find that the susceptibility distributions are narrow and unimodal, with MIC values between 0.5 and 4 mg/L for streptococci, enterococci and staphylococci. Linezolid entails mutation of the 23S rRNA that forms the binding site. Linezolid is an oxazolidinone whose mechanism of action involves inhibition of protein synthesis at a very early stage. Linezolid is added to 7H10 agar medium (Difco) supplemented with OADC (oleic acid, albumin, dextrose, and catalase) at 50°C to 56°C by doubling the dilutions to yield a final concentration of 0.125 μg/mL to 4 μg/mL. Linezolid shows excellent in vitro activity against all the strains tested (MICs ≤ 1 μg/ml), including those resistant to SIRE. Cell Assay: Linezolid was a potent inhibitor of cell-free transcription-translation in E. coli. IC50 was 1.8 mM. linezolid MICs vary slightly owing to the different test method and laboratory. The MIC values were between 0.5 and 4 mg/L for streptococci, enterococci and staphylococci.
In VivoClinical Trials: Linezolid is fully bioavailable following oral administration, with maximum plasma linezolid concentrations achieved between 1 and 2 hours after oral administration. The elimination half-life of linezolid is 5–7 hours, and twice-daily administration of 400–600mg provides steady-state concentrations in the therapeutic range.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.9643 mL14.8214 mL29.6428 mL59.2856 mL
5mM0.5929 mL2.9643 mL5.9286 mL11.8571 mL
10mM0.2964 mL1.4821 mL2.9643 mL5.9286 mL
20mM0.1482 mL0.7411 mL1.4821 mL2.9643 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.