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BTZ043

Cat. No. M1689
BTZ043 Structure
Synonym:

BTZ038, BTZ044

Size Price Availability Quantity
10mM*1mL in DMSO USD 95  USD95 In stock
5mg USD 88  USD88 In stock
10mg USD 120  USD120 In stock
50mg USD 385  USD385 In stock
100mg USD 640  USD640 In stock
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Quality Control & Documentation
Biological Activity

BTZ043 (BTZ038, BTZ044) is a decaprenylphosphoryl-b-D-ribose 2-epimerase inhibitor. BTZ043 (BTZ038, BTZ044) is an enzyme which produces the cell wall of the pathogenic bacterium Mycobacterium tuberculosis. The MIC of BTZ043 racemate against M. tuberculosis H37Rv and Mycobacterium smegmatis were 1 ng/ml and 4 ng/ml, respectively.

Customer Product Validations & Biological Datas
Source Antimicrob Agents Chemother (2012). Figure 2. BTZ043
Method
Cell Lines M. tuberculosis H37Rv
Concentrations 0.375 ng/ml
Incubation Time 6 days
Results The data clearly show that under these conditions there is no longer any synergy between BTZ043 and TMC207, suggesting that inhibition of DprE1 is essential for the interaction.
Source Antimicrob Agents Chemother (2012). Figure 1. BTZ043
Method resazurin checkerboard assay
Cell Lines M. tuberculosis H37Rv
Concentrations 0.375 ng/ml
Incubation Time 6 days
Results Compound interactions were evaluated by growing H37Rv in sub-MIC fractions of BTZ043 in combination with sub-MIC fractions of various front-line and experimental anti-TB compounds.
Protocol (for reference only)
Cell Experiment
Cell lines macrophages infected with GFP-labeled M. tuberculosis
Preparation method Intracellular activity of BTZ.
Raw 264.7 macrophages (ATCC # TIB-71) (1.5 x 108 cells) were infected with H37Rv-GFP at an MOI of 1:1 in 300 ml of RPMI 1640 (Gibco) with 10% heat-inactivated fetal calf serum (Gibco) for 2 h at 37 °C with shaking (100 rpm). For each compound, a series of 16 two-fold dilutions in quadruplicate was tested. Infected cells were then incubated in the presence of the compound for 5 days at 37 °C, 5% CO2. Then, macrophages were stained with SYTO 60 (Invitrogen, S11342) followed by plate sealing and image acquisition. Confocal images were recorded on an automated fluorescent confocal microscope OperaTM (PerkinElmer) using a 20X-water objective (NA 0.70). Mycobacteria-GFP are detected using a 488-nm laser coupled with a 535/50 nm detection filter (green channel, GFP excitation) and cells labeled with Syto 60 are identified with 635-nm laser coupled with a 690/40 nm detection filter (red channel, Syto 60 excitation).
Concentrations 0~1 μ M
Incubation time 5 days
Animal Experiment
Animal models M. tuberculosis H37Rv infected BALB/c mice chronical model
Formulation carboxymethyl cellulose formulation (0.25%)
Dosages 37.5 or 300 mg/kg once daily, six times/week for four weeks
Administration gavage
Chemical Information
Molecular Weight 431.39
Formula C17H16F3N3O5S
CAS Number 957217-65-1
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Makarov V, et al. Science. Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis.

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Keywords: BTZ043, BTZ038, BTZ044 supplier, Anti-infection, inhibitors, activators


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