PA-824

Catalog No.S1162

PA-824 is an anti-tuberculosis drug for tuberculosis with MIC less than 2.8 μM.Phase 2.

Price Stock Quantity  
USD 210 In stock
USD 270 In stock
USD 970 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

PA-824 Chemical Structure

PA-824 Chemical Structure
Molecular Weight: 359.26

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

PA-824 is available in the following compound libraries:

Product Information

Product Description

Biological Activity

Description PA-824 is an anti-tuberculosis drug for tuberculosis with MIC less than 2.8 μM.Phase 2.
Targets tuberculosis [1]
In vitro In vitro, PA-824 exhibits the high activity against multidrug-resistant clinical isolates from Asia (India and South Korea) and from throughout the United States (MIC < 1 μg/ml) and is equally active against the drug-sensitive and multidrug-resistant isolates of M. tuberculosis (MICs range, 0.039 to 0.531 μg/ml). [1] A recent study shows that single-nucleotide polymorphisms of PA-824 resistance genes (fgd1 [Rv0407] and ddn [Rv3547]) don't significantly affect the PA-824 MICs (≤ 0.25 μg/ml). [2]
In vivo In the rapid tuberculosis mouse model, PA-824 shows significant anti-microbial activity in a dose-dependent manner: at 50 mg/kg, PA-824 in MC produces a more than 1-log reduction of the CFU in the lungs; at 100 mg/kg it produces about a 2-log reduction, and at 300 mg/kg it produces a 3-log reduction. Furthermore, long-term treatment of PA-824 at 100 mg/kg in cyclodextrin/lecithin also leads to the reduction of the bacterial load below 500 CFU in the lungs and spleen. [1] PA-824 exhibits time-dependent anti-microbial activity in a murine model of tuberculosis with a maximal observed bactericidal effect of 0.1 log CFU/day over 24 days. [3]
Features An experimental anti-tuberculosis drug.

Protocol(Only for Reference)

Cell Assay: [1]

Cell lines M. tuberculosis H37Rv
Concentrations 2.0 μg/mL - 8.0 pg/mL
Incubation Time 21 days
Method A method is used to determine the MICs by a microdilution plate assay by using M. tuberculosis H37Rv. INH is dissolved in sterile, double-distilled water at a stock concentration of 500 μg/ml. PA-824 is dissolved in 100% dimethyl sulfoxide (DMSO) to a stock concentration of 100 μg/ml. A 1:2 dilution series of both compounds is made in a separate 96-well microtiter plate by using the same diluents. The interior 60 wells of a 96-well round-bottom microtiter assay plate are seeded with 98 μl of bacterial suspension. Two microliters of each drug is transferred to the assay plate wells containing bacteria. The final concentrations of INH in the wells range from 10.0 to 0.039 μg/mL; the final concentrations of PA-824 range from 2.0 μg/mL to 8.0 pg/mL. The assay plates are incubated at 37 °C for at least 21 days and are observed every 3 to 4 days to evaluate changes in growth. Inhibition of growth is determined both by visual examination and with a spectrophotometer at an OD600.

Animal Study: [1]

Animal Models Gamma interferon gene-disrupted (GKO) mice are infected via a low-dose aerosol exposure to M. tuberculosis Erdman.
Formulation PA-824 is formulated either in 0.5% methylcellulose (MC) or in cyclodextrin/lecithin (CM2).
Dosages ≤300 mg/kg
Administration Administered via p. o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Lenaerts AJ, et al. Antimicrob Agents Chemother. 2005, 49(6), 2294-2301.

[2] Feuerriegel S, et al. Antimicrob Agents Chemother. 2011, 55(12), 5718-5722.

view more

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-05-29)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02422524 Suspended Tuberculosis National Institute of Allergy and Infectious Diseases (NI  ...more National Institute of Allergy and Infectious Diseases (NIAID) September 2015 Phase 1
NCT02256696 Suspended Pulmonary Tuberculosis Johns Hopkins University April 2015 Phase 2
NCT02333799 Recruiting Pulmonary Tuberculosis Global Alliance for TB Drug Development March 2015 Phase 3
NCT02342886 Suspended Tuberculosis, Pulmonary, Drug Sensitive|Tuberculosis, Pulmonary, Multi Drug-resistant Global Alliance for TB Drug Development February 2015 Phase 3
NCT02193776 Active, not recruiting Tuberculosis Global Alliance for TB Drug Development November 2014 Phase 2

view more

Chemical Information

Download PA-824 SDF
Molecular Weight (MW) 359.26
Formula

C14H12F3N3O5

CAS No. 187235-37-6
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 72 mg/mL (200.41 mM)
Ethanol 16 mg/mL (44.53 mM)
Water <1 mg/mL (<1 mM)
In vivo 0.5% methylcellulose 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name (S)-6-(4-(trifluoromethoxy)benzyloxy)-2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related Others Products

  • CB-839

    CB-839 is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. Phase 1.

  • GKT137831

    GKT137831 is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectively. Phase 2.

  • LB-100

    LB-100 is a water soluble protein phosphatase 2A (PP2A) inhibitor. Phase 1.

  • Puromycin 2HCl

    Puromycin 2HCl is an aminonucleoside antibiotic, which acts as a protein synthesis inhibitor.

  • Cyclosporin A

    Cyclosporin A is an immunosuppressive agent, binds to the cyclophilin and then inhibits calcineurin with IC50 of 7 nM in a cell-free assay, widely used in organ transplantation to prevent rejection.

  • Cyclophosphamide Monohydrate

    Cyclophosphamide Monohydrate is a nitrogen mustard alkylating agent, it attaches the alkyl group to the guanine base of DNA.

  • Ganciclovir

    Ganciclovir is an antiviral drug for feline herpesvirus type-1 with IC50 of 5.2 μM in a cell-free assay.

  • Calcitriol

    Calcitriol is the hormonally active form of vitamin D.

  • Ribavirin

    Ribavirin, a synthetic guanosine analogue, possesses a broad spectrum of activity against DNA and RNA viruses.

  • BAPTA-AM

    BAPTA-AM is a selective, membrane-permeable calcium chelator.

Recently Viewed Items

Tags: buy PA-824 | PA-824 supplier | purchase PA-824 | PA-824 cost | PA-824 manufacturer | order PA-824 | PA-824 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us