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重要文件

PZ0014

Sigma-Aldrich

利奈唑胺

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

同義詞:

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

經驗公式(希爾表示法):
C16H20FN3O4
CAS號碼:
分子量::
337.35
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

產品名稱

利奈唑胺, ≥98% (HPLC)

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to off-white

溶解度

DMSO: >20 mg/mL

儲存溫度

room temp

SMILES 字串

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 密鑰

TYZROVQLWOKYKF-ZDUSSCGKSA-N

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相關類別

一般說明

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。

應用

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。

象形圖

Health hazard

訊號詞

Danger

危險聲明

危險分類

STOT RE 1 Oral

標靶器官

Bone

儲存類別代碼

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

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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Katherine S Long et al.
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During active tuberculosis a spectrum of physiologically different Mycobacterium tuberculosis bacilli reside in human tissues. Subpopulations of the pathogen survive antibiotic treatment for a prolonged time in a dormant state of phenotypic drug resistance, a phenomenon independent of genetic mutations.
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Four methicillin-resistant coagulase-negative staphylococci (MRCoNS), one Staphylococcus haemolyticus and three Staphylococcus cohnii, from infections of humans collected via the Ministry of Health National Antimicrobial Resistance Surveillance Net (Mohnarin) program in China were identified as linezolid-resistant. These four isolates were negative
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)
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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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