Linezolid (Synonyms: 利奈唑胺; PNU-100766)

目录号: HY-10394 纯度: 99.95%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Linezolid (PNU-100766) 是恶唑烷酮类合成抗生素的第一成员，通过抑制细菌蛋白质合成的起始而起作用，具有抗感染作用。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Linezolid Chemical Structure

CAS No. : 165800-03-3

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥605	In-stock
1 mg	￥171	In-stock
5 mg	￥343	In-stock
10 mg	￥550	In-stock
25 mg	￥1000	In-stock
50 mg	￥1800	In-stock
100 mg	￥3000	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

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生物活性
纯度 & 产品资料
参考文献

生物活性

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

细胞效力
(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]

体外研究
(In Vitro)

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

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

Clinical Trial

分子量

337.35

Formula

C₁₆H₂₀FN₃O₄

CAS 号

165800-03-3

性状

固体

颜色

White to off-white

中文名称

利奈唑胺

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 100 mg/mL (296.43 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	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

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.41 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.41 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.41 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

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

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.95%

选择批次：

Data Sheet (625 KB) SDS (418 KB)

COA (285 KB) LCMS (264 KB)

产品使用指南 (1538 KB)

参考文献

[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]

Linezolid 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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

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:

Linezolid165800-03-3PNU-100766利奈唑胺PNU100766PNU 100766BacterialAntibioticInhibitorinhibitorinhibit

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Linezolid (Synonyms: 利奈唑胺; PNU-100766)

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MCE 顾客使用本产品发表的 30 篇科研文献

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Linezolid (Synonyms: 利奈唑胺; PNU-100766)

Customer Review

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