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Linezolid [165800-03-3]

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Referencia HY-10394-100mg

embalaje : 100mg

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Teléfono : +1 850 650 7790

Marca : MedChemExpress

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Contact local distributor :

Teléfono : +1 850 650 7790

Descripciòn

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.

Solvente y solubilidad

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
10 mM	0.2964 mL	1.4821 mL	2.9643 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.

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureza y Documentación

Purity: 99.95%

Ficha de datos (275 KB) SDS (418 KB)

COA (248 KB) LCMS (264 KB)

Instrucciones de manejo (2659 KB)

Referencias

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

[2]. Chiappini E, Conti C, Galli L et al. Clinical efficacy and tolerability of linezolid in pediatric patients: a systematic review. Clin Ther. 2010 Jan;32(1):66-88. [Content Brief]

[3]. Perry CM, Jarvis B. Linezolid: a review of its use in the management of serious gram-positive infections. Drugs. 2001;61(4):525-51. [Content Brief]

[4]. He MZ, Jiang YW, Cai C. Mechanisms and epidemiology of linezolid resistance in staphylococci.Zhonghua Jie He He Hu Xi Za Zhi. 2012 May;35(5):360-2. [Content Brief]

[5]. Karau MJ, Tilahun AY, Schmidt SM, Clark CR, Patel R, Rajagopalan G. Linezolid is Superior to Vancomycin in Experimental Pneumonia Caused by Superantigen-Producing Staphylococcus aureus in HLA class II Transgenic Mice. Antimicrob Agents Chemother. 2012 Jul 30. [Content Brief]

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Linezolid [165800-03-3]

Referencia HY-10394-100mg

Contact local distributor :

Marca : MedChemExpress

Contact local distributor :

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