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Ethambutol

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Chemical Structure| 74-55-5 同义名 : Emb
CAS号 : 74-55-5
货号 : A939026
分子式 : C10H24N2O2
纯度 : 98%
分子量 : 204.31
MDL号 : MFCD00242828
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Ethambutol (EMB) is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases. Antibacterial Ethambutol directly affects two polymers, arabinogalactan (AG) and lipoarabinomannan (LAM) in Mycobacterium smegmatis. In M. smegmatis, Ethambutol inhibits synthesis of arabinan completely and inhibits AG synthesis most likely as a consequence of this; more than 50% of the cell arabinan is released from the bacteria following Ethambutol treatment, whereas no galactan is released. Ethambutol main targets against embB gene product in M. avium. Ethambutol induces 60% changes in the embB gene in M. tuberculosis resistant mutants[3]. Combination of ethambutol and sparfloxacin has significant activity intracellularly and in animal models against M. avium and M. tuberculosis[4]. Pupillary constriction and dilation velocities were significantly decreased in patients with EMB-induced optic neuropathy, compared to normal controls[5]. Ethambutol usage is associated with permanent visual loss and should be avoided if possible or used with caution and proper ophthalmological follow-up[6]. The EON (Ethambutol-induced optic neuropathy) is a reversible optic neuropathy if the ocular toxicity is monitored closely among the tuberculosis patients that take ethambutol[7].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01222338 Tuberculosis Phase 2 Completed - Ukraine ... 展开 >> Lisichansk TB Dispensary Lisichansk, Luhansk, Ukraine, 20001 收起 <<
NCT02365623 Tuberculosis, Multidrug-Resist... 展开 >>ant 收起 << Phase 2 Active, not recruiting September 12, 2020 Japan ... 展开 >> Kiyose, Japan Sakai, Japan 收起 <<
NCT00000796 HIV Infections ... 展开 >> Tuberculosis 收起 << Not Applicable Completed - United States, Illinois ... 展开 >> Cook County Hosp Chicago, Illinois, United States, 60612 United States, Michigan Henry Ford Hosp Detroit, Michigan, United States, 48202 United States, New York Bronx Lebanon Hosp Ctr Bronx, New York, United States, 10456 Bronx Municipal Hosp Ctr/Jacobi Med Ctr Bronx, New York, United States, 10461 Comprehensive Health Care Ctr / Bronx Municipal Hosp Bronx, New York, United States, 10461 Montefiore Drug Treatment Ctr / Bronx Municipal Hosp Bronx, New York, United States, 10461 Montefiore Family Health Ctr / Bronx Municipal Hosp Bronx, New York, United States, 10461 Samaritan Village Inc / Bronx Municipal Hosp Bronx, New York, United States, 10461 Jack Weiler Hosp / Bronx Municipal Hosp Bronx, New York, United States, 10465 Montefiore Med Ctr / Bronx Municipal Hosp Bronx, New York, United States, 10467 North Central Bronx Hosp / Bronx Municipal Hosp Bronx, New York, United States, 10467 Interfaith Med Ctr Brooklyn, New York, United States, 112032098 SUNY / Health Sciences Ctr at Brooklyn Brooklyn, New York, United States, 112032098 Beth Israel Med Ctr New York, New York, United States, 10003 Clinical Directors Network of Region II New York, New York, United States, 10011 Bellevue Hosp / New York Univ Med Ctr New York, New York, United States, 10016 Saint Clare's Hosp and Health Ctr New York, New York, United States, 10019 Cornell Univ Med Ctr New York, New York, United States, 10021 Mount Sinai Med Ctr New York, New York, United States, 10029 Columbia Presbyterian Med Ctr New York, New York, United States, 100323784 Harlem AIDS Treatment Group / Harlem Hosp Ctr New York, New York, United States, 10037 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.89mL

0.98mL

0.49mL

24.47mL

4.89mL

2.45mL

48.95mL

9.79mL

4.89mL
参考文献

[1]Kaur D, Khuller GK. In vitro, ex-vivo and in vivo activities of ethambutol and sparfloxacin alone and in combination against mycobacteria. Int J Antimicrob Agents. 2001 Jan;17(1):51-5.

[2]Rastogi N, Labrousse V, et al. In vitro activities of fourteen antimicrobial agents against drug susceptible and resistant clinical isolates of Mycobacterium tuberculosis and comparative intracellular activities against the virulent H37Rv strain in human macrophages. Curr Microbiol. 1996 Sep;33(3):167-75.

[3]Ethambutol. Tuberculosis (Edinb). 2008 Mar;88(2):102-5

[4]Kaur D, Khuller GK. In vitro, ex-vivo and in vivo activities of ethambutol and sparfloxacin alone and in combination against mycobacteria. Int J Antimicrob Agents. 2001 Jan;17(1):51-5

[5]Yoo YJ, Hwang JM, Yang HK. Pupillary light reflex in ethambutol-induced optic neuropathy. Sci Rep. 2020 Dec 10;10(1):21601

[6]Lim SA. Ethambutol-associated optic neuropathy. Ann Acad Med Singap. 2006 Apr;35(4):274-8

[7]Song W, Si S. The rare ethambutol-induced optic neuropathy: A case-report and literature review. Medicine (Baltimore). 2017 Jan;96(2):e5889