Name: Linezolid (PNU-100766)
Brand: Selleck Chemicals
SKU: S1408
Availability: InStock
Rating: 5 (22 reviews)

Jump to

Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	Integrase Bacterial Anti-infection Fungal Antiviral COVID-19 Parasite Reverse Transcriptase HIV HCV Protease
Other Antibiotics Inhibitors	G418 Sulfate (Geneticin) Puromycin Nanchangmycin Sitafloxacin Hydrate Fusidine Gamithromycin Thiamphenicol Tildipirosin Spiramycin Nadifloxacin

Solubility

In vitro
Batch:

DMSO : 68 mg/mL (201.57 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%PEG400 1 0.5%Tween80 2 5%propylene glycol Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (88.93mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O to adjust the volume. to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	337.35	Formula	C₁₆H₂₀FN₃O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	165800-03-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

In vitro

Linezolid (PNU-100766) is an oxazolidinone, a new class of antibacterial agents with enhanced activity against pathogens. It inhibits initiation complex formation with either the 30S or the 70S ribosomal subunits from Escherichia coli, and also inhibits complex formation with Staphylococcus aureus 70S tight-couple ribosomes. This compound is a potent inhibitor of cell-free transcription-translation in E. coli, exhibiting 50% inhibitory concentrations (IC50s) of 1.8 mM. Its 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. The mechanism of action involves inhibition of protein synthesis at a very early stage, and entails mutation of the 23S rRNA that forms the binding site. It 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.

References

[1] https://pubmed.ncbi.nlm.nih.gov/9835522/
[2] https://pubmed.ncbi.nlm.nih.gov/9333037/
[3] https://pubmed.ncbi.nlm.nih.gov/10428937/

[4] https://pubmed.ncbi.nlm.nih.gov/12730138/
[5] https://pubmed.ncbi.nlm.nih.gov/12499228/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05944445	Recruiting	Thrombocytopenia; Drugs	Helwan University	July 13 2023	--
NCT05571722	Not yet recruiting	Antibiotic Prophylaxis\|General Surgery	Assistance Publique Hopitaux De Marseille	April 3 2023	Phase 4
NCT06291181	Completed	Staphylococcus Aureus	Sohag University	January 1 2023	Not Applicable
NCT05381194	Recruiting	Multidrug- and Rifampicin-resistant Tuberculosis	Asan Medical Center\|Pusan National University Hospital\|Samsung Medical Center\|Seoul National University Hospital\|Severance Hospital\|Chonnam National University Hospital\|The Catholic University of Korea\|Chungbuk National University Hospital\|Ulsan University Hospital\|Soon Chun Hyang University\|Incheon St.Mary''s Hospital\|DongGuk University\|National Medical Center Seoul	December 13 2022	Phase 4
NCT05801484	Recruiting	Side-effect of Antibiotic\|Efficacy\|Pharmacokinetics\|Critical Illness\|Intensive Care Unit ICU	Cluj Municipal Clinical Hospital\|Iuliu Hatieganu University of Medicine and Pharmacy	July 1 2022	Not Applicable

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Linezolid (PNU-100766) Antibiotics chemical

Chemical Structure

Molecular Weight: 337.35