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

Name: Pretomanid
Brand: MedChemExpress
SKU: HY-10844
Rating: 5.0 (11 reviews)

Cat. No.: HY-10844 Purity: 99.91%: Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 187235-37-6

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
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200 mg	Get quote
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Pretomanid:

11 Publications Citing Use of MCE Pretomanid

Cell Proliferation/Viability Assay

Flow Cytometry

: 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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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

Tuberculosis.

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	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]
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	> 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	> 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]

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

Molecular Weight

359.26

Formula

C₁₄H₁₂F₃N₃O₅

CAS No.

187235-37-6

Appearance

Solid

Color

Off-white to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.91%

Select Batch:

Data Sheet (274 KB) SDS (394 KB)

COA (248 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[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

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

Pretomanid Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pretomanid187235-37-6PA-824 (S)-PA 824PA824PA 824BacterialAntibioticInhibitorinhibitorinhibit

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

Customer Review

Other Forms of Pretomanid:

Pretomanid Related Antibodies

11 Publications Citing Use of MCE Pretomanid

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•Related Screening Libraries:

•Related Small Molecules:

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View All Antibiotic Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Pretomanid Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Pretomanid Related Classifications

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