Radezolid (Synonyms: 雷得唑来; RX-1741)

目录号: HY-14800 纯度: 98.06%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Radezolid (RX-1741) 是一种噁唑烷酮类抗生素。Radezolid 对葡萄球菌，衣原体和军团菌具有活性，对 Linezolid 耐药菌株也具有活性。

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

Radezolid Chemical Structure

CAS No. : 869884-78-6

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1739	In-stock
1 mg	￥718	In-stock
5 mg	￥1581	In-stock
10 mg	￥2660	In-stock
50 mg	￥5300	In-stock
100 mg		询价
200 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 10 篇科研文献

: Radezolid purchased from MCE. Usage Cited in: Br J Cancer. 2021 Mar 24. [Abstract]; Radezolid (10-50μM; 48 hours) treatment significantly reduces the expression of YAP1 target genes (both at protein and mRNA level) in H357CisR and SCC-9 CisR cells.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Radezolid (RX-1741) is a oxazolidinone antibiotic. Radezolid is active against Staphylococcus, Chlamydia, and Legionella species, and remains active against Linezolid-resistant strains^[1]^[2].

IC₅₀ & Target

Oxazolidinone

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
THP-1	EC₅₀	0.02 mg/L Compound: Radezolid	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	0.04 mg/L Compound: Radezolid	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	0.07 mg/L Compound: Radezolid	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	0.09 mg/L Compound: Radezolid	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	0.09 mg/L Compound: Radezolid	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	0.12 mg/L Compound: Radezolid	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	0.14 mg/L Compound: Radezolid	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	0.16 mg/L Compound: Radezolid	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	0.24 mg/L Compound: Radezolid	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	0.24 mg/L Compound: Radezolid	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	0.29 mg/L Compound: Radezolid	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	0.31 mg/L Compound: Radezolid	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	0.47 mg/L Compound: Radezolid	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]
THP-1	EC₅₀	1.51 mg/L Compound: Radezolid	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]

体外研究
(In Vitro)

Radezolid MICs are systematically equal to or lower (up to 3 log2 dilutions) than those of linezolid for all linezolid-susceptible strains, with an 8-fold difference for the linezolid-resistant strains. Radezolid shows a greater potency than linezolid, independent of the bacteria tested, when concentrations are expressed on a weight (mg/L) basis. Radezolid shows an improved potency compared to that of linezolid when concentrations are expressed on a weight (mg/L) basis^[1]. Radezolid and TR-700 perform well against 3-copy G2447T, G2576T, and G2576T/T2571C mutants^[2].

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

Clinical Trial

分子量

438.45

Formula

C₂₂H₂₃FN₆O₃

CAS 号

869884-78-6

性状

固体

颜色

White to off-white

中文名称

雷得唑来

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 25 mg/mL (57.02 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	2.2808 mL	11.4038 mL	22.8076 mL
5 mM	0.4562 mL	2.2808 mL	4.5615 mL
10 mM	0.2281 mL	1.1404 mL	2.2808 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

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 (5.70 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 (5.70 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 (5.70 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）。

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: 99.27%

选择批次：

Data Sheet (626 KB) SDS (251 KB)

COA (195 KB) HNMR (290 KB) LCMS (126 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Lemaire S, et al. Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila. [Content Brief]

[2]. Locke JB, et al. Structure-activity relationships of diverse oxazolidinones for linezolid-resistant Staphylococcus aureus strains possessing the cfr methyltransferase gene or ribosomal mutations. Antimicrob Agents Chemother. 2010 Dec;54(12):5337-43. [Content Brief]

Cell Assay ^[1]	Antibiotic accumulation is determined following the general procedure, and the cellular content of [¹⁴C]radezolid is assayed in cell lysates by liquid scintillation counting (lowest limit of detection, 0.003 mg/liter; linear response between 0.01 and 0.78 mg/liter; R2=0.999). All cell drug contents are expressed by reference to the total cell protein content and converted into apparent total cell concentrations using a conversion factor of 5 μL per mg of cell protein. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Lemaire S, et al. Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila. [Content Brief] [2]. Locke JB, et al. Structure-activity relationships of diverse oxazolidinones for linezolid-resistant Staphylococcus aureus strains possessing the cfr methyltransferase gene or ribosomal mutations. Antimicrob Agents Chemother. 2010 Dec;54(12):5337-43. [Content Brief]

Cell Assay
^[1]

Antibiotic accumulation is determined following the general procedure, and the cellular content of [¹⁴C]radezolid is assayed in cell lysates by liquid scintillation counting (lowest limit of detection, 0.003 mg/liter; linear response between 0.01 and 0.78 mg/liter; R2=0.999). All cell drug contents are expressed by reference to the total cell protein content and converted into apparent total cell concentrations using a conversion factor of 5 μL per mg of cell protein.

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

参考文献

[1]. Lemaire S, et al. Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila. [Content Brief]

[2]. Locke JB, et al. Structure-activity relationships of diverse oxazolidinones for linezolid-resistant Staphylococcus aureus strains possessing the cfr methyltransferase gene or ribosomal mutations. Antimicrob Agents Chemother. 2010 Dec;54(12):5337-43. [Content Brief]

Radezolid 相关分类

Infection

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	2.2808 mL	11.4038 mL	22.8076 mL	57.0190 mL
	5 mM	0.4562 mL	2.2808 mL	4.5615 mL	11.4038 mL
	10 mM	0.2281 mL	1.1404 mL	2.2808 mL	5.7019 mL
	15 mM	0.1521 mL	0.7603 mL	1.5205 mL	3.8013 mL
	20 mM	0.1140 mL	0.5702 mL	1.1404 mL	2.8510 mL
	25 mM	0.0912 mL	0.4562 mL	0.9123 mL	2.2808 mL
	30 mM	0.0760 mL	0.3801 mL	0.7603 mL	1.9006 mL
	40 mM	0.0570 mL	0.2851 mL	0.5702 mL	1.4255 mL
	50 mM	0.0456 mL	0.2281 mL	0.4562 mL	1.1404 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:

Radezolid869884-78-6RX-1741雷得唑来RX1741RX 1741BacterialAntibioticInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

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上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Radezolid (Synonyms: 雷得唑来; RX-1741)

Customer Review

MCE 顾客使用本产品发表的 10 篇科研文献