Pyrazinamide
Based on 4 publication(s) in Google Scholar
Pyrazinamide (Pyrazinecarboxamide; Pyrazinoic acid amide) is a potent and orally active antitubercular antibiotic. Pyrazinamide is a proagent that is converted to the active form pyrazinoic acid (POA) by PZase/nicotinamidase encoded by the pncA gene in M. tuberculosis.
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- Reinheit: 99.93%
- CAS. Nr.: 98-96-4
- Formel: C5H5N3O
- Molecular Weight:123.11
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Speicherung:
Store at room temperature 3 years.
In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) Pyrazinamide
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Biologische Aktivität
IC50: Mycobacterium tuberculosis[1]
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Cell Line
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Type | Value | Description | References |
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| HepG2 | IC50 |
79.1 mM
Compound: PZA
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Cytotoxicity against human HepG2 cells
Cytotoxicity against human HepG2 cells
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[PMID: 23237840] |
| HepG2 | IC50 |
>1000 μM
Compound: PZA
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Cytotoxicity against human HepG2 cells assessed as inhibition of cell viability
Cytotoxicity against human HepG2 cells assessed as inhibition of cell viability
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[PMID: 37423128] |
| Vero | IC50 |
>50 μg/mL
Compound: Pyrazinamide
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Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay
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[PMID: 24044875] |
| Vero | IC50 |
>62.5 μg/mL
Compound: Pyrazinamide
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Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay
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[PMID: 24721315] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 98-96-4
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Appearance Solid
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Molecular Weight 123.11
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Formel C5H5N3O
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Color White to off-white
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SMILES
O=C(C1=NC=CN=C1)N
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Synonyms
Pyrazinecarboxamide; Pyrazinoic acid amide
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Store at room temperature 3 years
In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Antimicrob Agents Chemother
Incorporation of macrophage immune stresses into an intracellular assay of drug tolerance in Mycobacterium tuberculosis. [Abstract]2025 Sep 11:e0079525. PMID: 40934365 -
ACS Chem Biol
Investigate Natural Product Indolmycin and the Synthetically Improved Analogue Toward Antimycobacterial Agents. [Abstract]2022 Jan 21;17(1):39-53. PMID: 34908399 -
J Biochem Mol Toxicol
Network Toxicology and Molecular Docking Analysis of Antituberculosis Drug-Induced Hepatotoxicity. [Abstract]2025 Nov;39(11):e70602. PMID: 41215592 -
Res Sq
2024 Sep 2:rs.3.rs-4926508. PMID: 39281866
Lösungsmittel & Löslichkeit
DMSO : ≥ 50 mg/mL (406.14 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 6.67 mg/mL (54.18 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (20.31 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (20.31 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 27.5 mg/mL (223.38 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 8.1228 mL | 40.6141 mL | 81.2282 mL | 203.0704 mL |
| 5 mM | 1.6246 mL | 8.1228 mL | 16.2456 mL | 40.6141 mL | |
| 10 mM | 0.8123 mL | 4.0614 mL | 8.1228 mL | 20.3070 mL | |
| 15 mM | 0.5415 mL | 2.7076 mL | 5.4152 mL | 13.5380 mL | |
| 20 mM | 0.4061 mL | 2.0307 mL | 4.0614 mL | 10.1535 mL | |
| 25 mM | 0.3249 mL | 1.6246 mL | 3.2491 mL | 8.1228 mL | |
| 30 mM | 0.2708 mL | 1.3538 mL | 2.7076 mL | 6.7690 mL | |
| 40 mM | 0.2031 mL | 1.0154 mL | 2.0307 mL | 5.0768 mL | |
| 50 mM | 0.1625 mL | 0.8123 mL | 1.6246 mL | 4.0614 mL | |
| DMSO | 60 mM | 0.1354 mL | 0.6769 mL | 1.3538 mL | 3.3845 mL |
| 80 mM | 0.1015 mL | 0.5077 mL | 1.0154 mL | 2.5384 mL | |
| 100 mM | 0.0812 mL | 0.4061 mL | 0.8123 mL | 2.0307 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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