|5-氧代-4,5-二氢吡嗪-2-羧酸|CsnPharm

CAS No.: 34604-60-9

5-Hydroxypyrazine-2-Carboxylic Acid Catalog No. CSN23330

Synonyms: 5-Oxo-4,5-dihydropyrazine-2-carboxylic acid

5-Hydroxypyrazine-2-Carboxylic acid, a metabolite of pyrazinamide, is versatile building block for synthesis of antituberculous agents.

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技术信息

生物活性

描述5-Hydroxypyrazine-2-Carboxylic Acid, a metabolite of anti-tuberculosis drug pyrazinamide (PZA). The PZA metabolite pyrazinoic acid (PA) is the active compound against M. tuberculosis. PZA and caffeine, in various doses (PZA=50 or 100 mg kg(-1) and caffeine= 0, 50, 100, and 150 mg kg(-1)), were administered to female Sprague-Dawley rats. PZA and its three main metabolites were quantified in 24 h urine samples by reversed phase-HPLC Concomitant administration of 100 mg kg(-1) caffeine and 50 mg kg(-1) PZA increased from the excretion (p<0.05) of the most water-soluble and the least toxic PZA metabolite 5-hydroxypyrazinoic acid (5-OH-PA) from 66.18+/-10.87 to 94.56+/-8.65 micromol/24 h. This effect was more pronounced when 100 mg kg(-1) of PZA was administered increasing excretion of 5-OH-PA from 113.28+/-70 to 173.23+/-17.82 micromol/24 h^[1]. 5OH-PYCA dissociates in two steps, with the corresponding dissociation constants pK (a1)=3.42 and pK (a2)=7.96, designating 5OH-PYCA as a medium weak acid^[2].
参考文献

[1] Mehmedagic A, Verite P, Menager S, et al. Investigation of the effects of concomitant caffeine administration on the metabolic disposition of pyrazinamide in rats. Biopharm Drug Dispos. 2002;23(5):191‐195
[2] Sak-Bosnar M, Kovar K. Acid-base characterization of 5-hydroxypyrazine-2-carboxylic acid and the role of ionic equilibria in the optimization of some process conditions for its biocatalytic production. Anal Bioanal Chem. 2005;383(3):539‐545

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 7.1378 mL
- 35.6888 mL
- 71.3776 mL
- 5 mM
- 1.4276 mL
- 7.1378 mL
- 14.2755 mL
- 10 mM
- 0.7138 mL
- 3.5689 mL
- 7.1378 mL

技术信息

CAS号

34604-60-9

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C5H4N2O3

运输

蓝冰

分子量

140.10

别名

5-Oxo-4,5-dihydropyrazine-2-carboxylic acid

溶解度

DMSO	50.0 mg/mL (356.9 mM) warming
Water	4.0 mg/mL (28.6 mM) warming

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