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异烟肼 /Isoniazid {[allProObj[0].p_purity_real_show]}

货号:A432881 同义名: 吡啶-4-酰肼 / INH;Isonicotinic acid hydrazide

Isonicotinic acid hydrazide is an antibacterial agent used primarily as a tuberculostatic by blocking the action of fatty acid synthase by interacting with KatG.

Isoniazid 化学结构 CAS号:54-85-3
Isoniazid 化学结构
CAS号:54-85-3
Isoniazid 3D分子结构
CAS号:54-85-3
Isoniazid 化学结构 CAS号:54-85-3
Isoniazid 3D分子结构 CAS号:54-85-3
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Isoniazid 纯度/质量文件 产品仅供科研

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Isoniazid 生物活性

描述 Isoniazid (INH) functions as a proagent that requires activation by a specific bacterial enzyme called catalase-peroxidase, named KatG in Mycobacterium tuberculosis, to exert its effects. It is bactericidal against rapidly dividing mycobacteria, exhibiting anti-tuberculostatic activity, but acts as a bacteriostatic agent against slow-growing mycobacteria[1].[2].[3].[4].
体外研究

Isoniazid (INH) is a prodrug and must be activated by a bacterial catalase-peroxidase enzyme that in M. tuberculosis is called KatG[1].

Isoniazid is bactericidal to rapidly dividing mycobacteria but is bacteriostatic if the mycobacteria are slow-growing[4].

作用机制 Isonicotinic acid hydrazide (INH) passively enters mycobacterial cell through the cell wall and is activated by a mycobacterial enzyme called KatG. Activated IHN led to the accumulation of reactive oxygen species. The produced isonicotinoyl radical binds to a NAD molecule, resulting in the inhibition of FASII enoyl-ACP reductase InhA, which is essential in the mycolic acid biosynthesis pathway. The inhibition impedes cell wall synthesis, and eventually leads to cell death.

Isoniazid 动物研究

Dose Rat: 0.05 g/kg[3] (s.c.)
Administration s.c.

Isoniazid 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
NCT02114684 Recurrent Tuberculosis Phase 1 Phase 2 Completed - South Africa ... 展开 >> CAPRISA eThekwini Clinical Research Site (eCRS) Durban, KwaZulu Natal, South Africa, 4001 收起 <<
NCT00018083 Tuberculosis ... 展开 >>HIV Infections 收起 << Not Applicable Unknown - United States, North Carolina ... 展开 >> Duke University Medical Center Recruiting Durham, North Carolina, United States, 27710 Contact: Carol D Hamilton, M.D.    919-684-3279 收起 <<
NCT02381470 Tuberculosis Phase 2 Not yet recruiting March 2018 Philippines ... 展开 >> Lung Center Philippines Not yet recruiting Manila, Philippines Contact: Vincent Balanag          Principal Investigator: Vincent Balanag          Philippines Tuberculosis Society (Quezon Institute) Not yet recruiting Manila, Philippines Contact: Jubert Benedicto          Principal Investigator: Jubert Benedicto          Singapore Changi General Hospital Not yet recruiting Singapore, Singapore Contact: Augustine Tee          Principal Investigator: Augustine Tee          National University Hospital, Singapore Not yet recruiting Singapore, Singapore Contact: Meera Gurumurthy    +65 6772 7861    meera@nuhs.edu.sg    Principal Investigator: Nicholas Paton 收起 <<

Isoniazid 参考文献

[1]Suarez, J., et al., An oxyferrous heme/protein-based radical intermediate is catalytically competent in the catalase reaction of Mycobacterium tuberculosis catalase-peroxidase (KatG). J Biol Chem, 2009. 284(11): p. 7017-29.

[2]Timmins, G.S., et al., Nitric oxide generated from isoniazid activation by KatG: source of nitric oxide and activity against Mycobacterium tuberculosis. Antimicrob Agents Chemother, 2004. 48(8): p. 3006-9.

[3]Singh, R., et al., PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release. Science, 2008. 322(5906): p. 1392-5.

[4]Ahmad, Z., et al., Biphasic kill curve of isoniazid reveals the presence of drug-tolerant, not drug-resistant, Mycobacterium tuberculosis in the guinea pig. J Infect Dis, 2009. 200(7): p. 1136-43.

Isoniazid 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

7.29mL

1.46mL

0.73mL

36.46mL

7.29mL

3.65mL

72.92mL

14.58mL

7.29mL

Isoniazid 技术信息

CAS号54-85-3
分子式C6H7N3O
分子量 137.14
别名 吡啶-4-酰肼 ;INH;Isonicotinic acid hydrazide;Isoniazid, Isonicotinylhydrazide, Hydra, Hyzyd, Isovit, Nydrazid;NSC 9659;Isonicotinylhydrazide;Isonicotinic hydrazide
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 50 mg/mL(364.59 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 30 mg/mL(218.75 mM),配合低频超声助溶

动物实验配方
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