1. Anti-infection
  2. Bacterial Antibiotic
  3. Linezolid

Linezolid (PNU-100766) is the first member of the class of oxazolidinone synthetic antibiotic. Linezolid acts by inhibiting the initiation of bacterial protein synthesis. Linezolid is used for the treatment of serious infections caused by Gram-positive bacteria that are resistant to several other antibiotics.

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

Linezolid Chemical Structure

Linezolid Chemical Structure

CAS No. : 165800-03-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 30 publication(s) in Google Scholar

Other Forms of Linezolid:

Top Publications Citing Use of Products

30 Publications Citing Use of MCE Linezolid

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Linezolid (PNU-100766) is the first member of the class of oxazolidinone synthetic antibiotic. Linezolid acts by inhibiting the initiation of bacterial protein synthesis. Linezolid is used for the treatment of serious infections caused by Gram-positive bacteria that are resistant to several other antibiotics[1][2][3].

IC50 & Target

Oxazolidinone

 

Cellular Effect
Cell Line Type Value Description References
CHO IC50
105.4 μM
Compound: linezolid
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
[PMID: 23812503]
H9c2 IC50
7.98 μM
Compound: Linezolid
Inhibition of mitochondrial protein synthesis in rat H9c2 cells measured after 5 days by ELISA
Inhibition of mitochondrial protein synthesis in rat H9c2 cells measured after 5 days by ELISA
[PMID: 32666789]
H9c2 IC50
8.71 μM
Compound: Linezolid
Inhibition of mitochondrial protein synthesis in rat H9c2 cells after 5 days by In-Cell ELISA
Inhibition of mitochondrial protein synthesis in rat H9c2 cells after 5 days by In-Cell ELISA
[PMID: 28523106]
HEK293-A IC50
215 μg/mL
Compound: 1; LZN
Cytotoxicity against HEK293A cells after 48 hrs by MTT assay
Cytotoxicity against HEK293A cells after 48 hrs by MTT assay
10.1039/C5MD00101C
HeLa IC50
> 100 μg/mL
Compound: Linezolid
Cytotoxicity against human HeLa cells by MTT assay
Cytotoxicity against human HeLa cells by MTT assay
[PMID: 17456595]
HeLa IC50
> 400 μg/mL
Compound: Linezolid
Inhibition of metabolic activity in HeLa cells assessed as MTT reduction after 48 hrs
Inhibition of metabolic activity in HeLa cells assessed as MTT reduction after 48 hrs
[PMID: 17088489]
HepG2 IC50
> 25 μM
Compound: Linezolid
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31654879]
HepG2 IC50
> 25 μM
Compound: 1
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
[PMID: 30553735]
HepG2 IC50
> 25 μM
Compound: 1; Zyvox
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
[PMID: 30218910]
HepG2 EC50
> 30 μM
Compound: Linezolid
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by CellTiter-Glo assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by CellTiter-Glo assay
[PMID: 31383589]
L02 IC50
213 μg/mL
Compound: 1; LZN
Cytotoxicity against human L02 cells after 48 hrs by MTT assay
Cytotoxicity against human L02 cells after 48 hrs by MTT assay
10.1039/C5MD00101C
MG-63 IC50
> 400 μg/mL
Compound: Linezolid
Inhibition of metabolic activity in MG63 cells assessed as MTT reduction after 48 hrs
Inhibition of metabolic activity in MG63 cells assessed as MTT reduction after 48 hrs
[PMID: 17088489]
NIH3T3 IC50
465 μg/mL
Compound: Linezolid
Cytotoxicity against mouse NIH/3T3 cells after 24 hrs by MTT assay
Cytotoxicity against mouse NIH/3T3 cells after 24 hrs by MTT assay
[PMID: 19819597]
Osteoblast IC50
> 400 μg/mL
Compound: Linezolid
Antiproliferative effect against primary human osteoblasts assessed as BrdU incorporation into DNA after 48 hrs
Antiproliferative effect against primary human osteoblasts assessed as BrdU incorporation into DNA after 48 hrs
[PMID: 17088489]
Osteoblast IC50
> 400 μg/mL
Compound: Linezolid
Inhibition of metabolic activity in primary human osteoblasts assessed as MTT reduction after 48 hrs
Inhibition of metabolic activity in primary human osteoblasts assessed as MTT reduction after 48 hrs
[PMID: 17088489]
THP-1 EC50
0.18 mg/L
Compound: Linezolid
Antimicrobial activity against linezolid-susceptible Staphylococcus aureus SA238 infected in THP-1 cells at pH 5.5 after 24 hrs
Antimicrobial activity against linezolid-susceptible Staphylococcus aureus SA238 infected in THP-1 cells at pH 5.5 after 24 hrs
[PMID: 20385852]
THP-1 EC50
0.29 mg/L
Compound: Linezolid
Antimicrobial activity against linezolid-resistant Staphylococcus aureus SA238L infected in THP1 cells after 24 hrs
Antimicrobial activity against linezolid-resistant Staphylococcus aureus SA238L infected in THP1 cells after 24 hrs
[PMID: 20385852]
THP-1 EC50
0.35 mg/L
Compound: Linezolid
Antimicrobial activity against linezolid-susceptible Staphylococcus aureus SA238 infected in THP1 cells at pH 7.4 after 24 hrs
Antimicrobial activity against linezolid-susceptible Staphylococcus aureus SA238 infected in THP1 cells at pH 7.4 after 24 hrs
[PMID: 20385852]
THP-1 EC50
0.4 mg/L
Compound: Linezolid
Antimicrobial activity against linezolid-susceptible Staphylococcus aureus NRS384 infected in THP1 cells after 24 hrs
Antimicrobial activity against linezolid-susceptible Staphylococcus aureus NRS384 infected in THP1 cells after 24 hrs
[PMID: 20385852]
THP-1 EC50
0.47 mg/L
Compound: Linezolid
Antimicrobial activity against linezolid-susceptible Staphylococcus aureus ATCC 33591 infected in THP1 cells after 24 hrs
Antimicrobial activity against linezolid-susceptible Staphylococcus aureus ATCC 33591 infected in THP1 cells after 24 hrs
[PMID: 20385852]
THP-1 EC50
0.62 mg/L
Compound: Linezolid
Antimicrobial activity against Listeria monocytogenes infected in THP1 cells after 24 hrs
Antimicrobial activity against Listeria monocytogenes infected in THP1 cells after 24 hrs
[PMID: 20385852]
THP-1 EC50
0.63 mg/L
Compound: Linezolid
Antimicrobial activity against Staphylococcus aureus infected in THP1 cells after 24 hrs
Antimicrobial activity against Staphylococcus aureus infected in THP1 cells after 24 hrs
[PMID: 20385852]
THP-1 EC50
0.63 mg/L
Compound: Linezolid
Antimicrobial activity against linezolid-susceptible Staphylococcus aureus ATCC 25923 infected in THP1 cells after 24 hrs
Antimicrobial activity against linezolid-susceptible Staphylococcus aureus ATCC 25923 infected in THP1 cells after 24 hrs
[PMID: 20385852]
THP-1 EC50
0.63 mg/L
Compound: Linezolid
Antimicrobial activity against linezolid-susceptible Staphylococcus aureus SA040 infected in THP1 cells after 24 hrs
Antimicrobial activity against linezolid-susceptible Staphylococcus aureus SA040 infected in THP1 cells after 24 hrs
[PMID: 20385852]
THP-1 EC50
0.7 mg/L
Compound: Linezolid
Antimicrobial activity against linezolid-susceptible Staphylococcus aureus SA238 infected in THP1 cells after 24 hrs
Antimicrobial activity against linezolid-susceptible Staphylococcus aureus SA238 infected in THP1 cells after 24 hrs
[PMID: 20385852]
THP-1 EC50
0.84 mg/L
Compound: Linezolid
Antimicrobial activity against linezolid-susceptible Staphylococcus aureus NRS18 infected in THP1 cells after 24 hrs
Antimicrobial activity against linezolid-susceptible Staphylococcus aureus NRS18 infected in THP1 cells after 24 hrs
[PMID: 20385852]
THP-1 EC50
2.78 mg/L
Compound: Linezolid
Antimicrobial activity against linezolid-resistant Staphylococcus aureus SA040L infected in THP1 cells after 24 hrs
Antimicrobial activity against linezolid-resistant Staphylococcus aureus SA040L infected in THP1 cells after 24 hrs
[PMID: 20385852]
THP-1 EC50
2.99 mg/L
Compound: Linezolid
Antimicrobial activity against Staphylococcus epidermidis infected in THP1 cells after 24 hrs
Antimicrobial activity against Staphylococcus epidermidis infected in THP1 cells after 24 hrs
[PMID: 20385852]
THP-1 EC50
8.45 mg/L
Compound: Linezolid
Antimicrobial activity against Legionella pneumophila ATCC 33153 infected in THP1 cells after 48hrs
Antimicrobial activity against Legionella pneumophila ATCC 33153 infected in THP1 cells after 48hrs
[PMID: 20385852]
Vero IC50
> 200 μg/mL
Compound: Linezolid
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 30145051]
Vero IC50
> 64 μg/mL
Compound: Linezolid
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
[PMID: 32666789]
Vero IC50
> 64 μg/mL
Compound: Linezolid
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

Linezolid (PNU-100766) prevents the synthesis of bacterial protein via binding to rRNA on both the 30S and 50S ribosomal subunits[3].

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

Clinical Trial
Molecular Weight

337.35

Formula

C16H20FN3O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O[C@H]1CNC(C)=O)N(C1)C2=CC(F)=C(N3CCOCC3)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (296.43 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9643 mL 14.8214 mL 29.6428 mL
5 mM 0.5929 mL 2.9643 mL 5.9286 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.95%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9643 mL 14.8214 mL 29.6428 mL 74.1070 mL
5 mM 0.5929 mL 2.9643 mL 5.9286 mL 14.8214 mL
10 mM 0.2964 mL 1.4821 mL 2.9643 mL 7.4107 mL
15 mM 0.1976 mL 0.9881 mL 1.9762 mL 4.9405 mL
20 mM 0.1482 mL 0.7411 mL 1.4821 mL 3.7054 mL
25 mM 0.1186 mL 0.5929 mL 1.1857 mL 2.9643 mL
30 mM 0.0988 mL 0.4940 mL 0.9881 mL 2.4702 mL
40 mM 0.0741 mL 0.3705 mL 0.7411 mL 1.8527 mL
50 mM 0.0593 mL 0.2964 mL 0.5929 mL 1.4821 mL
60 mM 0.0494 mL 0.2470 mL 0.4940 mL 1.2351 mL
80 mM 0.0371 mL 0.1853 mL 0.3705 mL 0.9263 mL
100 mM 0.0296 mL 0.1482 mL 0.2964 mL 0.7411 mL
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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.

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Linezolid
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