Pyrazinamide 是一种有效的口服抗结核类抗生。

Pyrazinamide (Pyrazinecarboxamide; Pyrazinoic acid amide) is a potent and orally active antitubercular antibiotic. Pyrazinamide is a prodrug that is converted to the active form pyrazinoic acid (POA) by PZase/nicotinamidase encoded by the pncA gene in M. tuberculosis^[1][2].

IC50: Mycobacterium tuberculosis^[1]

Pyrazinamide exhibits remarkable activity in vivo activity, has no activity against growing Mycobacterium tuberculosis except at an acidic pH. In M. tuberculosis, acidic pH enhances the intracellular accumulation of pyrazinoic acid (POA), the active derivative of PZA.
POA is thought to disrupt membrane energetics and inhibit membrane transport function at acid pH in Mycobacterium tuberculosis^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

123.11

C₅H₅N₃O

98-96-4

吡嗪酰胺；羧酸胺；吡嗪甲酰胺

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 50 mg/mL (406.14 mM)

H₂O : 6.67 mg/mL (54.18 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： PBS

  Solubility: 27.5 mg/mL (223.38 mM); Clear solution; Need ultrasonic

• 2.

  请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

  Solubility: ≥ 2.5 mg/mL (20.31 mM); Clear solution

• 3.

  请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (20.31 mM); Clear solution

• 4.

  请依序添加每种溶剂： 10% DMSO 90% corn oil

  Solubility: ≥ 2.5 mg/mL (20.31 mM); Clear solution

• [1]. Y Zhang, et al. Role of acid pH and deficient efflux of pyrazinoic acid in unique susceptibility of Mycobacterium tuberculosis to pyrazinamide. J Bacteriol. 1999 Apr;181(7):2044-9. [Content Brief]

  [2]. Ying Zhang, et al. Mechanisms of Pyrazinamide Action and Resistance. Microbiol Spectr. 2014 Aug;2(4):MGM2-0023-2013. [Content Brief]