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Merck
CN

PZ0014

Sigma-Aldrich

利奈唑胺

≥98% (HPLC), powder, bacterial mRNA translation inhibitor

别名:

N-[[(5S)-3-[3-氟-4-(4-吗啉基)苯基] -2-氧代-5-恶唑烷基]甲基]乙酰胺, PNU-100766, U-100766

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About This Item

经验公式(希尔记法):
C16H20FN3O4
分子量:
337.35
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

产品名称

利奈唑胺, ≥98% (HPLC)

质量水平

方案

≥98% (HPLC)

表单

powder

颜色

white to off-white

溶解性

DMSO: >20 mg/mL

储存温度

room temp

SMILES字符串

CC(=O)NC[C@H]1CN(C(=O)O1)c2ccc(N3CCOCC3)c(F)c2

InChI

1S/C16H20FN3O4/c1-11(21)18-9-13-10-20(16(22)24-13)12-2-3-15(14(17)8-12)19-4-6-23-7-5-19/h2-3,8,13H,4-7,9-10H2,1H3,(H,18,21)/t13-/m0/s1

InChI key

TYZROVQLWOKYKF-ZDUSSCGKSA-N

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一般描述

利奈唑胺对多种革兰氏阳性菌具有抗菌活性,包括耐青霉素菌、耐甲氧西林菌和耐万古霉素菌。利奈唑胺可通过抑制起始复合物形成降低翻译反应速率,从而缩短新合成肽链长度。此外,它还有减少毒力因子的作用,可减少革兰氏阳性菌产生的毒素。

应用

利奈唑胺已用于棋盘式药物组合 MIC(最小抑制浓度)检测,以确定 ivacaftor是否与利奈唑胺的具有正相互作用。 已用于测定最低生物膜抑制浓度和用于治疗脓肿分枝杆菌感染的黑腹果蝇w1118。利奈唑胺已作为抗生素,研究它对大鼠肺部疟疾相关呼吸窘迫综合征(MAARDS)发生发展的影响。作为抗生素与黄苓素联用,研究它对耐甲氧西林金黄色葡萄球菌株的影响。作为抗生素,研究它对浮游生物生长和粪肠球菌生物膜形成的影响。

生化/生理作用

利奈唑胺是一种恶唑烷类抗菌药。它抑制细菌 mRNA的翻译和是一种弱的、可逆的、非选择性的单胺氧化酶抑制剂。
利奈唑胺是一种恶唑烷酮类抗菌药。 它与50S 亚基的细菌 23S 核糖体 RNA 上的位点结合,并阻止功能性 70S 起始复合物的形成,从而抑制细菌 mRNA 翻译。利奈唑胺也是一种弱的、可逆的非选择性单胺氧化酶抑制剂。

象形图

Health hazard

警示用语:

Danger

危险声明

危险分类

STOT RE 1 Oral

靶器官

Bone

储存分类代码

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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Binh An Diep et al.
The Journal of infectious diseases, 208(1), 75-82 (2013-03-28)
Linezolid is recommended for treatment of pneumonia and other invasive infections caused by methicillin-resistant Staphylococcus aureus (MRSA). The premise underlying this recommendation is that linezolid inhibits in vivo production of potent staphylococcal exotoxins, including Panton-Valentine leukocidin (PVL) and α-hemolysin (Hla)
D Clemett et al.
Drugs, 59(4), 815-827 (2000-05-10)
Linezolid is an oxazolidinone antibacterial agent that acts by inhibiting the initiation of bacterial protein synthesis. Cross-resistance between linezolid and other inhibitors of protein synthesis has not been demonstrated. Linezolid has a wide spectrum of activity against gram-positive organisms including
Katherine S Long et al.
Antimicrobial agents and chemotherapy, 56(2), 603-612 (2011-12-07)
Linezolid is an oxazolidinone antibiotic in clinical use for the treatment of serious infections of resistant Gram-positive bacteria. It inhibits protein synthesis by binding to the peptidyl transferase center on the ribosome. Almost all known resistance mechanisms involve small alterations
Seyed Mohammad Reza Hashemian et al.
Drug design, development and therapy, 12, 1759-1767 (2018-06-29)
Linezolid can be considered as the first member of the class of oxazolidinone antibiotics. The compound is a synthetic antibiotic that inhibits bacterial protein synthesis through binding to rRNA. It also inhibits the creation of the initiation complex during protein
Laura Morata et al.
Antimicrobial agents and chemotherapy, 57(4), 1913-1917 (2013-02-14)
Linezolid is an antibiotic with time-dependent activity, and both the percentage of time that plasma concentrations exceed the MIC and the area under the concentration-time curve over 24 h in the steady state divided by the MIC (AUC24/MIC ratio) are

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Bioactive small molecules for immune system signaling target identification/validation and antibiotics, antivirals, and antifungals offered.

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