Pretomanid
Based on 11 publication(s) in Google Scholar
Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
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- Pureza: 99.91%
- No. CAS: 187235-37-6
- Fòrmula: C14H12F3N3O5
- Peso molecular:359.26
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Publications Citing Use of MedChemExpress (MCE) Pretomanid
More- Int J Pharm. 2024 Aug 18:124608. [Abstract]
- Int J Pharm. 2024 Mar 25:653:123920. [Abstract]
- J Photochem Photobiol A Chem. 2024 Aug 1, 453, 115636.
- Nanomedicine. 2025 Apr;20(8):777-789. [Abstract]
- Molecules. 2024 Aug 26;29(17):4041. [Abstract]
- Antimicrob Agents Chemother. 2025 Sep 11:e0079525. [Abstract]
- mLife. 2025 Apr 15;4(2):155-168. [Abstract]
- ACS Infect Dis. 2021 Jan 8;7(1):141-152. [Abstract]
- Dis Model Mech. 2021 Dec 1;14(12):dmm049145. [Abstract]
- Infect Immun. 2026 Feb 9:e0057425. [Abstract]
- bioRxiv. 2025 Oct 17:2025.10.17.683099. [Abstract]
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Cell Proliferation/Viability Assay
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Flow Cytometry
Ver todos los productos específicos de isoformas Antibiotic
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Actividad biológica
Tuberculosis.
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | CC50 |
98 μM
Compound: 2
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Cytotoxicity against human HEK293 cells assessed as reduction in cell viability after 20 hrs
Cytotoxicity against human HEK293 cells assessed as reduction in cell viability after 20 hrs
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[PMID: 33151678] |
| HEK293 | IC50 |
>30 μM
Compound: 1, PA-824
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Inhibition of human Erg expressed in HEK293 cells by FAST patch clamp analysis
Inhibition of human Erg expressed in HEK293 cells by FAST patch clamp analysis
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[PMID: 22148391] |
| MRC5 | IC50 |
>64 μM
Compound: S-1; PA-824
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Cytotoxicity against human MRC5 cells after 72 hrs by resazurin dye based assay
Cytotoxicity against human MRC5 cells after 72 hrs by resazurin dye based assay
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[PMID: 29461823] |
| Vero | IC50 |
>100 μg/mL
Compound: PA824
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Cytotoxicity against african green monkey Vero cells after 72 hrs by MTS-PMS assay
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTS-PMS assay
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[PMID: 24087924] |
| Vero | IC50 |
>100 μM
Compound: 4; PA-824
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Cytotoxicity against African green monkey Vero cells assessed by reduction in cell viability incubated for 72 hrs by resazurin dye fluorescence based assay
Cytotoxicity against African green monkey Vero cells assessed by reduction in cell viability incubated for 72 hrs by resazurin dye fluorescence based assay
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[PMID: 34046598] |
| Vero | IC50 |
>125 μM
Compound: 1, PA-824
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Cytotoxicity against african green monkey Vero cells after 72 hrs by MTS assay
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTS assay
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[PMID: 19928920] |
| Vero | IC50 |
>128 μM
Compound: 1, PA-824
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Cytotoxicity against african green monkey Vero cells after 72 hrs by tetrazolium dye assay
Cytotoxicity against african green monkey Vero cells after 72 hrs by tetrazolium dye assay
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[PMID: 19968290] |
| Vero | IC50 |
>128 μM
Compound: 1, PA-824
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Cytotoxicity against African green monkey Vero cells after 72 hrs
Cytotoxicity against African green monkey Vero cells after 72 hrs
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[PMID: 26253632] |
| Vero | IC50 |
>128 μM
Compound: PA-824
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Cytotoxicity against african green monkey Vero cells after 72 hrs
Cytotoxicity against african green monkey Vero cells after 72 hrs
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[PMID: 21691438] |
| Vero | IC50 |
>128 μM
Compound: PA-824
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Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by CellTiter 96 assay
Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by CellTiter 96 assay
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[PMID: 24909079] |
| Vero | IC50 |
44 μg/mL
Compound: PA-824
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Cytotoxicity against African green monkey Vero cells by cell titer glo assay
Cytotoxicity against African green monkey Vero cells by cell titer glo assay
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[PMID: 26711150] |
Pretomanid (PA-824) showed significant activity at 2, 10, and 50 microg/ml, similar to that of metronidazole, in a dose-dependent manner[2].
Pretomanid (PA-824) has no effect on the viability of M. leprae in all three models, consistent with the lack of the nitroimidazo-oxazine-specific nitroreductase, encoded by Rv3547 in the M. leprae genome, which is essential for activation of this molecule[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pretomanid (PA-824) at 100 mg/kg in cyclodextrin/lecithin was as active as moxifloxacin at 100 mg/kg and isoniazid at 25 mg/kg and was slightly more active than rifampin at 20 mg/kg. Long-term treatment with Pretomanid (PA-824) at 100 mg/kg in cyclodextrin/lecithin reduced the bacterial load below 500 CFU in the lungs and spleen[2].
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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No. CAS 187235-37-6
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Appearance Solid
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Peso molecular 359.26
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Fòrmula C14H12F3N3O5
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Color Off-white to yellow
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SMILES
FC(F)(F)OC(C=C1)=CC=C1CO[C@@H]2COC3=NC([N+]([O-])=O)=CN3C2
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Synonyms
PA-824; (S)-PA 824
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (11)
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Journal Impact Factor
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Most Recent
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Int J Pharm
Development of a proliposomal pretomanid dry powder inhaler as a novel alternative approach for combating pulmonary tuberculosis. [Abstract]2024 Aug 18:124608. PMID: 39163929 -
Int J Pharm
A quality-by-design strategic approach for the development of bedaquiline-pretomanid nanoparticles as inhalable dry powders for TB treatment. [Abstract]2024 Mar 25:653:123920. PMID: 38387819 -
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Nanomedicine
3D spheroid model reveals enhanced efficacy of mannose-decorated nanoparticles for TB treatment. [Abstract]2025 Apr;20(8):777-789. PMID: 40099656 -
Molecules
Free Radical Production Induced by Nitroimidazole Compounds Lead to Cell Death in Leishmania infantum Amastigotes. [Abstract]2024 Aug 26;29(17):4041. PMID: 39274889
Pretomanid purchased from MedChemExpress. Usage Cited in: Molecules. 2024 Aug 26;29(17):4041. [Abstract]
viability data obtained from cells after 72 h of incubation in the presence of different concentrations of Pretomanid.
Pretomanid purchased from MedChemExpress. Usage Cited in: Molecules. 2024 Aug 26;29(17):4041. [Abstract]
Representative flow cytometry graphs showing ROS production by the axenic amastigote cultures of L. infantum-iRFP stained with DCFH-DA after the 0.28 μM Pretomanid.
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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 -
mLife
Identification of a phenyl ester covalent inhibitor of caseinolytic protease and analysis of the ClpP1P2 inhibition in mycobacteria. [Abstract]2025 Apr 15;4(2):155-168. PMID: 40313980 -
ACS Infect Dis
Two-Way Regulation of MmpL3 Expression Identifies and Validates Inhibitors of MmpL3 Function in Mycobacterium tuberculosis. [Abstract]2021 Jan 8;7(1):141-152. PMID: 33319550 -
Dis Model Mech
An anti-tuberculosis compound screen using a zebrafish infection model identifies an aspartyl-tRNA synthetase inhibitor. [Abstract]2021 Dec 1;14(12):dmm049145. PMID: 34643222 -
Infect Immun
Mouse models of tuberculosis uniformly featuring hypoxic necrotic lesions and poor response to chemotherapy. [Abstract]2026 Feb 9:e0057425. PMID: 41660838 -
bioRxiv
Mouse Models Uniformly Featuring Human-like Lesions Harboring Drug-tolerant Mycobacterium tuberculosis. [Abstract]2025 Oct 17:2025.10.17.683099. PMID: 41279700
Solvente y solubilidad
DMSO : 125 mg/mL (347.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 12.5 mg/mL (34.79 mM; Need ultrasonic)
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: 2.08 mg/mL (5.79 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.08 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (5.79 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Stover CK, et al. A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. Nature. 2000 Jun 22;405(6789):962-6. [Content Brief]
[2]. Lenaerts AJ, et al. Preclinical testing of the nitroimidazopyran PA-824 for activity against Mycobacterium tuberculosis in a series of in vitro and in vivo models. Antimicrob Agents Chemother. 2005 Jun;49(6):2294-301. [Content Brief]
[3]. Manjunatha UH, et al. Mycobacterium leprae is naturally resistant to PA-824. Antimicrob Agents Chemother. 2006 Oct;50(10):3350-4. [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 2.7835 mL | 13.9175 mL | 27.8350 mL | 69.5875 mL |
| 5 mM | 0.5567 mL | 2.7835 mL | 5.5670 mL | 13.9175 mL | |
| 10 mM | 0.2783 mL | 1.3917 mL | 2.7835 mL | 6.9587 mL | |
| 15 mM | 0.1856 mL | 0.9278 mL | 1.8557 mL | 4.6392 mL | |
| 20 mM | 0.1392 mL | 0.6959 mL | 1.3917 mL | 3.4794 mL | |
| 25 mM | 0.1113 mL | 0.5567 mL | 1.1134 mL | 2.7835 mL | |
| 30 mM | 0.0928 mL | 0.4639 mL | 0.9278 mL | 2.3196 mL | |
| DMSO | 40 mM | 0.0696 mL | 0.3479 mL | 0.6959 mL | 1.7397 mL |
| 50 mM | 0.0557 mL | 0.2783 mL | 0.5567 mL | 1.3917 mL | |
| 60 mM | 0.0464 mL | 0.2320 mL | 0.4639 mL | 1.1598 mL | |
| 80 mM | 0.0348 mL | 0.1740 mL | 0.3479 mL | 0.8698 mL | |
| 100 mM | 0.0278 mL | 0.1392 mL | 0.2783 mL | 0.6959 mL |
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