GLPBio

PA-824

Catalog No.: GC13561Purity:>99.50%Synonyms: Pretomanid
COASDSData Sheet
PA-824 is a nitroimidazole anti-tuberculosis drug. PA-824 kills bacteria by inhibiting Mycobacterium tuberculosis cell wall synthesis and interfering with energy metabolism.

Products are for research use only. Not for human use. We do not sell to patients.

PA-824
Cas No.: 187235-37-6
10mM (in 1mL DMSO)In Stock
$39.00
1
1mgIn Stock
$18.00
1
5mgIn Stock
$35.00
1
10mgIn Stock
$56.00
1
50mgIn Stock
$105.00
1
100mgIn Stock
$161.00
1
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    610, 366–372 (2022)
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    187(9):2288-2304 (2024)
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Description

PA-824 is a nitroimidazole anti-tuberculosis drug. PA-824 kills bacteria by inhibiting Mycobacterium tuberculosis cell wall synthesis and interfering with energy metabolism[1-2]. PA-824 can be used in research related to multidrug-resistant tuberculosis and extensively drug-resistant tuberculosis[3-4].

In vitro, PA-824 (2.5-10µg/ml) was used to treat M. leprae and M. tuberculosis for 7 days. PA-824 had no effect on the viability of M. leprae, PA-824 significantly reduced the proliferation of M. tuberculosis[5]. PA-824 (0.015-16µg/ml) was used to treat M. avium, M. intracellulare, M. abscessus, and M. massiliense for 3-14 days. The inhibitory effect of PA-824 on these five mycobacterial species was generally weak, with minimum inhibitory concentration (MIC) values all greater than 16µg/ml[6].

In vivo, PA-824 (200mg/kg/day) was administered by oral gavage to BALB/c mice infected with M. avium, M. abscessus, M. chelonae, or M. fortuitum (once daily, starting 7 days after infection, for 28 days). PA-824 demonstrated strong antibacterial activity in the lungs and spleens of mice infected with M. abscessus, and weak activity in the kidneys of mice infected with M. fortuitum. PA-824 showed no significant antibacterial effect in the mouse models infected with M. avium or M. chelonae[7]. PA-824 (40-80mg/kg/day) was administered by oral gavage to Tg.rasH2 mice (once daily for 26 weeks). The mice, exposed to PA-824 at levels exceeding the clinical human exposure dose, did not exhibit drug-related early death, tumors, or non-tumorigenic microscopic pathological changes[8].

References:
[1] Keam SJ. Pretomanid: First Approval. Drugs. 2019 Nov;79(16):1797-1803. doi: 10.1007/s40265-019-01207-9.
[2] Gils T, Lynen L, de Jong BC, et al. Pretomanid for tuberculosis: a systematic review. Clin Microbiol Infect. 2022 Jan;28(1):31-42.
[3] Deb U, Biswas S. Pretomanid: The latest USFDA-approved anti-tuberculosis drug. Indian J Tuberc. 2021 Apr;68(2):287-291.
[4] Koehler N, Andres S, Merker M, et al. Pretomanid-resistant tuberculosis. J Infect. 2023 May;86(5):520-524.
[5] Manjunatha UH, Lahiri R, Randhawa B, et al. Mycobacterium leprae is naturally resistant to PA-824. Antimicrob Agents Chemother. 2006 Oct;50(10):3350-4.
[6] Zheng H, Wang Y, He W, et al. In Vitro Activity of Pretomanid against Nontuberculous Mycobacteria. Antimicrob Agents Chemother. 2022 Jan 18;66(1):e0181021.
[7] Zheng L, Qi X, Zhang W, et al. Efficacy of PBTZ169 and pretomanid against Mycobacterium avium, Mycobacterium abscessus, Mycobacterium chelonae, and Mycobacterium fortuitum in BALB/c mice models. Front Cell Infect Microbiol. 2023 Mar 22;13:1115530.
[8] Ambroso JL, Dillberger J, Bruning-Barry R, et al. Assessment of the Carcinogenic Potential of Pretomanid in Transgenic Tg.rasH2 Mice. Int J Toxicol. 2022 Sep-Oct;41(5):367-379.

Protocol

Cell experiment [1]:

Cell lines

Mycobacterium tuberculosis, Mycobacterium leprae

Preparation Method

Resident peritoneal macrophages from Swiss mice were harvested and adhered. For M. leprae, macrophages were infected overnight with fresh, mouse-derived M. leprae at a multiplicity of infection (MOI) of 20:1 at 33°C. For M. tuberculosis, macrophages were infected with M. tuberculosis at an MOI of 2:1 for 30 min at 37°C. Infected macrophages were incubated with PA-824 (2.5-10μg/ml) in culture medium for 7 days. PA-824 was also tested in axenic BACTEC 7H12B medium with M. leprae.

Reaction Conditions

2.5-10μg/ml; 7 day.

Applications

PA-824 had no effect on the metabolic activity of M. leprae in either axenic culture or within infected macrophages. In contrast, in M. tuberculosis-infected macrophages, PA-824 treatment resulted in at least a 2-log (100-fold) reduction in colony-forming units.

Animal experiment [2]:

Animal models

BALB/c mice

Preparation Method

Mice were inoculated intravenously in the tail vein with M. avium, M. abscessus, M. chelonae, or M. fortuitum. Dexamethasone (5mg/kg; daily) was administered 1 week prior to infection and stopped 6 days after infection. Mice were treated with drugs for 28 days starting 7 days after infection. PA-824 (200mg/kg/day) was administered by gavage.

Dosage form

200mg/kg/day; Oral gavage; 28 days.

Applications

In M. abscessus-infected mice, PA-824 treatment significantly reduced the bacterial load in the lungs and spleen compared to the untreated control. In M. fortuitum-infected mice, PA-824 showed only weak activity in the kidneys. PA-824 showed no significant inhibitory effect against M. avium and had little activity against M. chelonae in mice.

References:
[1] Manjunatha UH, Lahiri R, Randhawa B, et al. Mycobacterium leprae is naturally resistant to PA-824. Antimicrob Agents Chemother. 2006 Oct;50(10):3350-4.
[2] Zheng L, Qi X, Zhang W, et al. Efficacy of PBTZ169 and pretomanid against Mycobacterium avium, Mycobacterium abscessus, Mycobacterium chelonae, and Mycobacterium fortuitum in BALB/c mice models. Front Cell Infect Microbiol. 2023 Mar 22;13:1115530.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
187235-37-6
Synonyms
Pretomanid
Chemical Name
(6S)-2-nitro-6-[[4-(trifluoromethoxy)phenyl]methoxy]-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine
SMILES
C1C(COC2=NC(=CN21)[N+](=O)[O-])OCC3=CC=C(C=C3)OC(F)(F)F
Molecular Formula
C14H12F3N3O5
Molecular Weight
359.26
Solubility
≥ 17.85mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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