Art. -Nr.: HY-10844

Pretomanid

(Synonyms: PA-824; (S)-PA 824)

11 Cited Publications

Kundenbewertung

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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Reinheit: 99.91%
CAS. Nr.: 187235-37-6
Formel: C₁₄H₁₂F₃N₃O₅
Molecular Weight:359.26

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Pretomanid Chemical Structure

CAS. Nr.: 187235-37-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (11)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Tuberculosis.

Alle Antibiotic Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	CC₅₀	98 μM Compound: 2	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	[PMID: 33151678]
HEK293	IC₅₀	>30 μM Compound: 1, PA-824	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	[PMID: 22148391]
MRC5	IC₅₀	>64 μM Compound: S-1; PA-824	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	[PMID: 29461823]
Vero	IC₅₀	>100 μg/mL Compound: PA824	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	[PMID: 24087924]
Vero	IC₅₀	>100 μM Compound: 4; PA-824	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	[PMID: 34046598]
Vero	IC₅₀	>125 μM Compound: 1, PA-824	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	[PMID: 19928920]
Vero	IC₅₀	>128 μM Compound: 1, PA-824	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	[PMID: 19968290]
Vero	IC₅₀	>128 μM Compound: 1, PA-824	Cytotoxicity against African green monkey Vero cells after 72 hrs Cytotoxicity against African green monkey Vero cells after 72 hrs	[PMID: 26253632]
Vero	IC₅₀	>128 μM Compound: PA-824	Cytotoxicity against african green monkey Vero cells after 72 hrs Cytotoxicity against african green monkey Vero cells after 72 hrs	[PMID: 21691438]
Vero	IC₅₀	>128 μM Compound: PA-824	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	[PMID: 24909079]
Vero	IC₅₀	44 μg/mL Compound: PA-824	Cytotoxicity against African green monkey Vero cells by cell titer glo assay Cytotoxicity against African green monkey Vero cells by cell titer glo assay	[PMID: 26711150]

In Vitro

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.

In Vivo

Pretomanid (PA-824) exhibited a sub-micromolar minimal inhibitory concentration (MIC) against MTB, Although Pretomanid (PA-824) was not the most potent NAP against cultured MTB clinical isolates, it was the most active in infected mice when orally administered at 25 mg/kg. This indicated that Pretomanid (PA-824) might possess more desirable pharmacokinetic properties than the other more potent NAP compounds that we tested. Further studies in mice at 25, 50 and 100 mg/kg Pretomanid (PA-824) daily for 10 days resulted in reductions of mycobacterial burden in both spleen and lung tissues that were comparable to that of INH at 25 mg/kg^[1].
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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 187235-37-6
Appearance Solid
Molecular Weight 359.26
Formel C₁₄H₁₂F₃N₃O₅
Color Off-white to yellow
SMILES

FC(F)(F)OC(C=C1)=CC=C1CO[C@@H]2COC3=NC([N+]([O-])=O)=CN3C2
Synonyms

PA-824; (S)-PA 824
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (11)

All Cell Proliferation/Viability AssayFlow Cytometry

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Journal Impact Factor

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
J Photochem Photobiol A Chem

2024 Aug 1, 453, 115636.
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.
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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7835 mL

13.9175 mL

27.8350 mL

5 mM

0.5567 mL

2.7835 mL

5.5670 mL

10 mM

0.2783 mL

1.3917 mL

2.7835 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.08 mg/mL (5.79 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.08 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Pretomanid

11 Cited Publications

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Pretomanid

Anti-Infection Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Antibacterial Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Antibiotics Library

Drug-Induced Liver Injury (DILI) Compound Library

Rare Diseases Drug Library

FDA-Approved Anticancer Drug Library

Off-patent Drug Library

Anti-tuberculosis Compound Library

Anti-Drug-Resistant Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Pretomanid

Alle Antibiotic Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Pretomanid

Anti-Infection Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Antibacterial Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Antibiotics Library

Drug-Induced Liver Injury (DILI) Compound Library

Rare Diseases Drug Library

FDA-Approved Anticancer Drug Library

Off-patent Drug Library

Anti-tuberculosis Compound Library

Anti-Drug-Resistant Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Pretomanid

Alle Antibiotic Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Pretomanid Related Classifications

Art. -Nr.: HY-10844