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BTZ043 Racemate

Catalog No.
A5118
DprE1 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$203.00
In stock
5mg
$120.00
In stock
10mg
$230.00
In stock
50mg
$680.00
In stock

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Background

MIC: 1 ng/ml (2.3 nM) for M. tuberculosis H37Rv and 4 ng/ml (9.2 nM) for Mycobacterium smegmatis

The loss of human lives to tuberculosis (TB) continues unabated as a result of poverty, synergy with the HIV/AIDS pandemic, and the emergence of multidrug- and extensively drug-resistant strains of Mycobacterium tuberculosis. BTZ043 is the most advanced candidate for inclusion in combination therapies for both drug-sensitive and extensively drug-resistant TB.

In vitro: BTZ043 displayed similar activity against all clinical isolates of M. tuberculosis that were tested, including extensively drug-resistant and multidrug-resistant strains, indicating that it targets a previously unknown biological function. BTZ043 is bactericidal, reducing viability in vitro by more than 1000-fold in under 72 hours, which is comparable to the INH killing effect [1].

In vivo: The in vivo efficacy of BTZ043 was assessed 4 weeks after a low-dose aerosol infection of in the chronic BALB/c mice model of TB. Four weeks of treatment with BTZ043 reduced the bacterial load in the lungs and spleens by 1 and 2 logs, respectively, at the concentrations used. Additional findings suggest that BTZ efficacy is time- rather than dose-dependent [1].

Clinical trial: Up to now, BTZ043 is still in the preclinical development stage.

Reference:
[1] Makarov V, Manina G, Mikusova K, et al.  Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis. Science. 2009 May 8;324(5928):801-4.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt431.39
Cas No.957217-65-1
FormulaC17H16F3N3O5S
Solubility≥10.4mg/mL in DMSO with gentle warming, ≥3.27 mg/mL in EtOH with ultrasonic and warming,insoluble in H2O
Chemical Name2-(3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one
SDFDownload SDF
Canonical SMILESCC1COC2(O1)CCN(CC2)C3=NC(=O)C4=CC(=CC(=C4S3)[N+](=O)[O-])C(F)(F)F
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description BTZ043 racemate is an inhibitor of decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1).
Targets DprE1          
IC50            

Quality Control

Quality Control & MSDS

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Chemical structure

BTZ043 Racemate

Related Biological Data

BTZ043 Racemate

Related Biological Data

BTZ043 Racemate