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Pyrazinamide

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Chemical Structure| 98-96-4 同义名 : 吡嗪-2-酰胺 ;Pyrazinoic acid amide;Pyrazinecarboxamide;NSC 14911;MK 56;α-Pyrazinamide;Aldinamide
CAS号 : 98-96-4
货号 : A132133
分子式 : C5H5N3O
纯度 : 98%
分子量 : 123.113
MDL号 : MFCD00006132
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(406.13 mM)，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: 6.5 mg/mL(52.8 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Pyrazinamide (PZA) is an important sterilising tuberculosis drug that helps to shorten the duration of current chemotherapy regimens for tuberculosis. PZA is more active against old than against actively growing cultures. The highly diverse mutations in the PZase gene (pncA) that lead to loss of PZase activity cause PZA resistance[2]. PZA markedly inhibited the activity of M. tuberculosis FASI (the eukaryotic-like fas1 gene), the biosynthesis of C16 to C24/C26 fatty acids from acetyl-CoA[3]. PZA is hydrolyzed intracellularly to pyrazinoic acid (POA) by pyrazinamidase (PZase, encoded by pncA), an enzyme frequently lost in PZA-resistant strains, but the target of POA in Mycobacterium tuberculosis has remained elusive[1]. In plant cells, PZA is converted to pyrazinecarboxylic acid (POA), suppressing the activity of 1-aminocyclopropane-1-carboxylic acid oxidase (ACO), the enzyme catalysing the final step of ethylene formation[4].
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
NCT01994460 Pulmonary Tuberculosis Without... 展开 >> Resistance to Rifampicin 收起 << Phase 2 Unknown June 2016 Korea, Republic of ... 展开 >> Seoul National University Bundang Hospital Recruiting Seongnam, Kyunggi, Korea, Republic of, 463-707 Contact: Jong Sun Park, MD    031-787-7054    jspark.im@gmail.com    Principal Investigator: Jong Sun Park, MD          National Medical Center Recruiting Seoul, Korea, Republic of, 100-799 Contact: Ji Yeon Lee, MD    82222607284    jedidiah125@gmail.com    Principal Investigator: Ji Yeon Lee, MD          SMG-SNU Boramae Medical Center Recruiting Seoul, Korea, Republic of, 156-707 Contact: Deog Kyeom Kim, MD    02-870-2228    kimdkmd@gmail.com    Principal Investigator: Deog Kyeom Kim, MD 收起 <<
NCT02958709 Tuberculosis, Meningeal Phase 1 Phase 2 Recruiting June 2019 India ... 展开 >> Byramji Jeejeebhoy Government Medical College and Sassoon Hospital Recruiting Pune, Maharashtra, India, 411001 Contact: Chhaya Valvi, MD       chhayavalvi@gmail.com    Contact: Vidya Mave, MD, MPH & TM    919503646148    vidyamave@gmail.com    National Institute of Research in TB and Institute of Child Health Not yet recruiting Chennai, Tamil Nadu, India, 600031 Contact: Bella Devaleenal, MBBS    919841746690    bella.d@nirt.res.in    Contact: Syed Hissar, MD, MPH    919442927242    syed.hissar@nirt.res.in    Malawi UNC Project- Malawi Not yet recruiting Lilongwe, Lilongwe District, Malawi Contact: Mina Hosseinipour, MD,MPH    2651750610    mina_hosseinipour@med.unc.edu    Contact: Tisungane Mvalo, MBBS, FCPaed    2651750610    tmvalo@unclilongwe.org 收起 <<
NCT02153528 Tuberculosis, Pulmonary Phase 3 Completed - Bangladesh ... 展开 >> Damien Foundation Bangladesh TB project in Greater Mymensingh district (8 selected clinics) Dhaka, Greater Mymensingh district, Bangladesh 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

8.12mL

1.62mL

0.81mL

40.61mL

8.12mL

4.06mL

81.23mL

16.25mL

8.12mL
参考文献

[1]Shi W, Zhang X, Jiang X, et al. Pyrazinamide inhibits trans-translation in Mycobacterium tuberculosis. Science. 2011;333(6049):1630–1632

[2]Zhang Y, Mitchison D. The curious characteristics of pyrazinamide: a review. Int J Tuberc Lung Dis. 2003;7(1):6–21

[3]Zimhony O, Cox JS, Welch JT, Vilchèze C, Jacobs WR Jr. Pyrazinamide inhibits the eukaryotic-like fatty acid synthetase I (FASI) of Mycobacterium tuberculosis. Nat Med. 2000;6(9):1043–1047

[4]Sun X, Li Y, He W, et al. Pyrazinamide and derivatives block ethylene biosynthesis by inhibiting ACC oxidase. Nat Commun. 2017;8:15758. Published 2017 Jun 12