GLPBio

PA-824

Catalog No.: GC13561Purity:>99.50%Synonyms: Pretomanid
COASDSData Sheet

PA-824 (PA-824) ist ein Antibiotikum, das für die Erforschung von multi-resistenten Tuberkulose-Bakterien verwendet wird, die die Lungen betreffen.

Die Produkte sind ausschließlich für Forschungszwecke bestimmt. Nicht zur Anwendung am Menschen. Wir verkaufen nicht an Patienten.

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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Zitate (Citations)

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    641, 529–536 (2025)
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    628, 630–638 (2024)
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    Nature
    632, 686–694 (2024)
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    Nature
    618, 1017–1023 (2023)
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    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
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    Science
    388(6745) (2025)
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    387(6739) (2025)
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    387(6734) (2025)
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    35, 97–116 (2025)
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    34, 683–706 (2024)
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    33, 273–287 (2023)
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    33, 546–561 (2023)
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    33, 904–922 (2023)
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    31, 1291–1307 (2021)

Beschreibung (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.

Protokoll (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.

Produktdokumente (Product Documents)

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
187235-37-6
Synonyme
Pretomanid
Chemischer 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
Summenformel
C14H12F3N3O5
Molekulargewicht
359.26
Löslichkeit
≥ 17.85mg/mL in DMSO
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

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