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Isoniazid

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Chemical Structure| 54-85-3 同义名 : 吡啶-4-酰肼 ;INH;Isonicotinic acid hydrazide;Isoniazid, Isonicotinylhydrazide, Hydra, Hyzyd, Isovit, Nydrazid;NSC 9659;Isonicotinylhydrazide;Isonicotinic hydrazide
CAS号 : 54-85-3
货号 : A432881
分子式 : C6H7N3O
纯度 : 98+%
分子量 : 137.14
MDL号 : MFCD00006426
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
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：
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].
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.
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 <<
实验方案
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
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.