PyrazinamideCAS# 98-96-4 |
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Quality Control & MSDS
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Chemical structure
3D structure
| Cas No. | 98-96-4 | SDF | Download SDF |
| PubChem ID | 1046 | Appearance | Powder |
| Formula | C5H5N3O | M.Wt | 123.11 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Pyrazinecarboxamide; Pyrazinoic acid amide | ||
| Solubility | DMSO : ≥ 50 mg/mL (406.14 mM) H2O : 6.67 mg/mL (54.18 mM; Need ultrasonic) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | pyrazine-2-carboxamide | ||
| SMILES | C1=CN=C(C=N1)C(=O)N | ||
| Standard InChIKey | IPEHBUMCGVEMRF-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C5H5N3O/c6-5(9)4-3-7-1-2-8-4/h1-3H,(H2,6,9) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Pyrazinamide is a pyrazine that is used therapeutically as an antitubercular agent.
Target: Antibacterial
Pyrazinamide is a prodrug that stops the growth of Mycobacterium tuberculosis. Pyrazinoic acid was thought to inhibit the enzyme fatty acid synthase (FAS) I, which is required by the bacterium to synthesise fatty acids although this has been discounted. It was also suggested that the accumulation of pyrazinoic acid disrupts membrane potential and interferes with energy production, necessary for survival of M. tuberculosis at an acidic site of infection. Pyrazinoic acid binds to the ribosomal protein S1 (RpsA) and inhibits trans-translation. This may explain the ability of the drug to kill dormant mycobacteria [1-4]. References: | |||||
Pyrazinamide Dilution Calculator
Pyrazinamide Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 8.1228 mL | 40.6141 mL | 81.2282 mL | 162.4563 mL | 203.0704 mL |
| 5 mM | 1.6246 mL | 8.1228 mL | 16.2456 mL | 32.4913 mL | 40.6141 mL |
| 10 mM | 0.8123 mL | 4.0614 mL | 8.1228 mL | 16.2456 mL | 20.307 mL |
| 50 mM | 0.1625 mL | 0.8123 mL | 1.6246 mL | 3.2491 mL | 4.0614 mL |
| 100 mM | 0.0812 mL | 0.4061 mL | 0.8123 mL | 1.6246 mL | 2.0307 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Pyrazinamide is a pyrazine that is used therapeutically as an antitubercular agent.
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Lung Tissue Concentrations of Pyrazinamide among Patients with Drug-Resistant Pulmonary Tuberculosis.[Pubmed:28373198]
Antimicrob Agents Chemother. 2017 May 24;61(6). pii: AAC.00226-17.
Improved knowledge regarding the tissue penetration of antituberculosis drugs may help optimize drug management. Patients with drug-resistant pulmonary tuberculosis undergoing adjunctive surgery were enrolled. Serial serum samples were collected, and microdialysis was performed using ex vivo lung tissue to measure Pyrazinamide concentrations. Among 10 patients, the median Pyrazinamide dose was 24.7 mg/kg of body weight. Imaging revealed predominant lung lesions as cavitary (n = 6 patients), mass-like (n = 3 patients), or consolidative (n = 1 patient). On histopathology examination, all tissue samples had necrosis; eight had a pH of Pyrazinamide concentrations within the recommended range of 20 to 60 mug/ml. The median lung tissue free Pyrazinamide concentration was 20.96 mug/ml. The median tissue-to-serum Pyrazinamide concentration ratio was 0.77 (range, 0.54 to 0.93). There was a significant inverse correlation between tissue Pyrazinamide concentrations and the amounts of necrosis (R = -0.66, P = 0.04) and acid-fast bacilli (R = -0.75, P = 0.01) identified by histopathology. We found good penetration of Pyrazinamide into lung tissue among patients with pulmonary tuberculosis with a variety of radiological lesion types. Our tissue pH results revealed that most lesions had a pH conducive to Pyrazinamide activity. The tissue penetration of Pyrazinamide highlights its importance in both drug-susceptible and drug-resistant antituberculosis treatment regimens.
Simultaneous Spectrophotometric Determination of Rifampicin, Isoniazid and Pyrazinamide in a Single Step.[Pubmed:28243267]
Iran J Pharm Res. 2016 Fall;15(4):713-723.
Three antituberculosis medications are investigated in this work consist of rifampicin, isoniazid and Pyrazinamide. The ultra violet (UV) spectra of these compounds are overlapped, thus use of suitable chemometric methods are helpful for simultaneous spectrophotometric determination of them. A generalized version of net analyte signal standard addition method (GNASSAM) was used for determination of three antituberculosis medications as a model system. In generalized net analyte signal standard addition method only one standard solution was prepared for all analytes. This standard solution contains a mixture of all analytes of interest, and the addition of such solution to sample, causes increases in net analyte signal of each analyte which are proportional to the concentrations of analytes in added standards solution. For determination of concentration of each analyte in some synthetic mixtures, the UV spectra of pure analytes and each sample were recorded in the range of 210 nm-550 nm. The standard addition procedure was performed for each sample and the UV spectrum was recorded after each addition and finally the results were analyzed by net analyte signal method. Obtained concentrations show acceptable performance of GNASSAM in these cases.
Population Pharmacokinetics of Pyrazinamide in Patients with Tuberculosis.[Pubmed:28289033]
Antimicrob Agents Chemother. 2017 May 24;61(6). pii: AAC.02625-16.
The current treatment used for tuberculosis (TB) is lengthy and needs to be shortened and improved. Pyrazinamide (PZA) has potent sterilizing activity and has the potential to shorten the TB treatment duration, if treatment is optimized. The goals of this study were (i) to develop a population pharmacokinetic (PK) model for PZA among patients enrolled in PK substudies of Tuberculosis Trial Consortium (TBTC) trials 27 and 28 and (ii) to determine covariates that affect PZA PK. (iii) We also performed simulations and target attainment analysis using the proposed targets of a maximum plasma concentration (Cmax) of >35 mug/ml or an area under the concentration-versus-time curve (AUC) of >363 mug . h/ml to see if higher weight-based dosing could improve PZA efficacy. Seventy-two patients participated in the substudies. The mean (standard deviation [SD]) Cmax was 30.8 (7.4) mug/ml, and the mean (SD) AUC from time zero to 24 h (AUC0-24) was 307 (83) mug . h/ml. A one-compartment open model best described PZA PK. Only body weight was a significant covariate for PZA clearance. Women had a lower volume of distribution (V/F) than men, and both clearance (CL/F) and V/F increased with body weight. Our simulations show that higher doses of PZA (>50 mg/kg of body weight) are needed to achieve the therapeutic target of an AUC/MIC of >11.3 in >80% of patients, while doses of >80 mg/kg are needed for target attainment in 90% of patients, given specific assumptions about MIC determinations. For the therapeutic targets of a Cmax of >35 mug/ml and/or an AUC of >363 mug . h/ml, doses in the range of 30 to 40 mg/kg are needed to achieve the therapeutic target in >90% of the patients. Further clinical trials are needed to evaluate the safety and efficacy of higher doses of PZA.
