1. Anti-infection
  2. Bacterial
    Antibiotic
  3. Pretomanid

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

Cat. No.: HY-10844 Purity: 99.53%
Handling Instructions

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.

Pretomanid Chemical Structure

Pretomanid Chemical Structure

CAS No. : 187235-37-6

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1  mL in DMSO USD 121 In-stock
Estimated Time of Arrival: December 31
10 mg USD 110 In-stock
Estimated Time of Arrival: December 31
50 mg USD 240 In-stock
Estimated Time of Arrival: December 31
100 mg USD 360 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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[1].

IC50 & Target

Tuberculosis.

In Vitro

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-1 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 [1]. Pretomanid (PA-824) showed significant activity at 2, 10, and 50 microg/ml, similar to that of metronidazole, in a dose-dependent manner. 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]. 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].

Clinical Trial
Molecular Weight

359.26

Formula

C₁₄H₁₂F₃N₃O₅

CAS No.

187235-37-6

SMILES

FC(F)(F)OC(C=C1)=CC=C1CO[[email protected]@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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (55.67 mM; ultrasonic and warming and heat to 80°C)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2 mg/mL (5.57 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2 mg/mL (5.57 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2 mg/mL (5.57 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.53%

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Keywords:

PretomanidPA-824(S)-PA 824PA824PA 824BacterialAntibioticInhibitorinhibitorinhibit

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