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

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

目錄號: HY-10394 純度: 99.95%
COA 產(chǎn)品使用指南

Linezolid (PNU-100766) 是惡唑烷酮類合成抗生素的第一成員,通過抑制細(xì)菌蛋白質(zhì)合成的起始而起作用,具有抗感染作用。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Linezolid Chemical Structure

Linezolid Chemical Structure

CAS No. : 165800-03-3

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10 mM * 1 mL in DMSO ¥605
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1 mg ¥171
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5 mg ¥343
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10 mg ¥550
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25 mg ¥1000
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50 mg ¥1800
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100 mg ¥3000
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Customer Review

Other Forms of Linezolid:

MCE 顧客使用本產(chǎn)品發(fā)表的 30 篇科研文獻(xiàn)

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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

 

細(xì)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]
體外研究
(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 號
性狀

固體

顏色

White to off-white

中文名稱

利奈唑胺

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

4°C, protect from light

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

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : ≥ 100 mg/mL (296.43 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí),請?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn):

請根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.41 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.41 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

    2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
動(dòng)物溶解方案計(jì)算器
請輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
請輸入您的動(dòng)物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括:DMSO ,均可在 MCE 網(wǎng)站選購。 Tween 80,均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。

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

您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水
連續(xù)給藥周期超過半月以上,請謹(jǐn)慎選擇該方案。
請確保第一步儲(chǔ)備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.95%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí),請?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱:
Linezolid
目錄號:
HY-10394
需求量: