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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
4°C, protect from light
- 英文名:
INH; Isonicotinic acid hydrazide; Isonicotinic hydrazide
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
54-85-3
- 规格:
10 mM * 1 mL/100 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥550.0 |
|---|---|---|---|
| 规格: | 100 mg | 产品价格: | ¥500.0 |
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Isoniazid
CAS No. : 54-85-3
MCE 国际站:Isoniazid
产品活性:Isoniazid (INH) 是一种前药,必须被细菌过氧化氢酶 KatG 激活。Isoniazid 对快速分裂的分枝杆菌具有杀菌作用,并具有抗菌活性。
研究领域:Anti-infection | Autophagy
作用靶点:Bacterial | Autophagy | Mitophagy
In Vitro: Isoniazid (INH) is a prodrug and must be activated by a bacterial catalase-peroxidase enzyme that in M. tuberculosis is called KatG.
KatG couples the isonicotinic acyl with NADH to form isonicotinic acyl-NADH complex. This complex binds tightly to the enoyl-acyl carrier protein reductase known as InhA, thereby blocking the natural enoyl-AcpM substrate and the action of fatty acid synthase. This process inhibits the synthesis of mycolic acid, required for the mycobacterial cell wall. A range of radicals are produced by KatG activation of isoniazid, including nitric oxide, which has also been shown to be important in the action of another antimycobacterial prodrug PA-824.
Isoniazid is bactericidal to rapidly dividing mycobacteria, but is bacteriostatic if the mycobacteria are slow-growing.
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文献和实验Phenotypic and Genotypic Characterization of N-Acetylation
Variation among the human population in the ability to acetylate drugs has been known since the observations on individual variations in isoniazid toxicity in the 1950s. The genetic basis for this was soon appreciated and has come to be known
) is used for M. tuberculosis complex identification; the use of a multiplex allele-specific PCR is demonstrated to detect the isoniazid resistance; PCR-sequencing assays are applied for rifampicin and ofloxacin resistance detection and 16S rDNA sequencing
异烟肼(isoniazid)是常用的抗结核药。在体内主要通过N-乙酰基转移酶(N-acetyltransferase,简称乙酰化酶)。将异烟肼转变为乙酰化异烟肼而灭活。按对异烟肼灭活的快慢,人群中可分出两类:一类称为快灭活者(rapid inactivator),血中异烟肼半减期为45-110分钟;另一类称为慢灭活者(slow inactivator),半减期2-4.5小时。而慢灭活者是由于乙酰化酶的遗传缺乏故灭活较慢。此酶系由常染色体一对等位基因控制。快灭活者(RR)与慢
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