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Merck
CN

PZ0014

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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关于此项目

经验公式(希尔记法):
C16H20FN3O4
化学文摘社编号:
分子量:
337.35
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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产品名称

利奈唑胺, ≥98% (HPLC)

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to off-white

solubility

DMSO: >20 mg/mL

storage temp.

room temp

SMILES string

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

General description

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。

Application

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。

Biochem/physiol Actions

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。


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pictograms

Health hazard

signalword

Danger

hcodes

Hazard Classifications

STOT RE 1 Oral

target_organs

Bone

存储类别

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

flash_point_f

Not applicable

flash_point_c

Not applicable



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商品

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


Giovanni Sotgiu et al.
The European respiratory journal, 40(6), 1430-1442 (2012-04-13)
Linezolid is used off-label to treat multidrug-resistant tuberculosis (MDR-TB) in absence of systematic evidence. We performed a systematic review and meta-analysis on efficacy, safety and tolerability of linezolid-containing regimes based on individual data analysis. 12 studies (11 countries from three
Gregory J Moran et al.
The Lancet. Infectious diseases, 14(8), 696-705 (2014-06-10)
New antibiotics are needed to treat infections caused by drug-resistant bacteria. Tedizolid is a novel oxazolidinone antibacterial drug designed to provide enhanced activity against Gram-positive pathogens. We aimed to assess the efficacy and safety of intravenous to oral tedizolid for
Bing Gu et al.
The Journal of antimicrobial chemotherapy, 68(1), 4-11 (2012-09-06)
The oxazolidinone antibiotic linezolid has demonstrated potent antimicrobial activity against Gram-positive bacterial pathogens, including methicillin-resistant staphylococci. This article systematically reviews the published literature for reports of linezolid-resistant Staphylococcus (LRS) infections to identify epidemiological, microbiological and clinical features for these infections.



全球贸易项目编号

货号GTIN
PZ0014-25MG04061835304837
PZ0014-5MG04061836687359