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