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BTZ043 Racemate Catalog No.GC18127

DprE1 inhibitor

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10mM (in 1mL DMSO)
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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 957217-65-1 SDF
Chemical Name 2-(3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one
Canonical SMILES CC1COC2(O1)CCN(CC2)C3=NC(=O)C4=CC(=CC(=C4S3)[N+](=O)[O-])C(F)(F)F
Formula C17H16F3N3O5S M.Wt 431.39
Solubility ≥10.4mg/mL in DMSO with gentle warming, ≥3.27 mg/mL in EtOH with ultrasonic and warming, <1.19 mg/mL in H2O Storage Store at -20°C
General tips For 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.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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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.

[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.