BTZ043 Racemate
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.
- 1. ANNANYA SHETTY. "ANALYSIS OF MYCOBACTERIAL CELL ENVELOPE STRESS AND DISCOVERY OF A NOVEL MMPL3 INHIBITOR." NATIONAL UNIVERSITY OF SINGAPORE.2018.
- 2. Zhengquan Xu, Wei Peng, et al. "In vitro interactions between R207910 and second-line anti-TB drugs or BTZ043 against mycobacterium tuberculosis by microplate alamar blue assay." Int J Clin Exp Med 2016;9(3):6336-6341.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 431.39 |
Cas No. | 957217-65-1 |
Formula | C17H16F3N3O5S |
Solubility | insoluble in H2O; ≥10.4 mg/mL in DMSO with gentle warming; ≥3.27 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 2-(3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one |
SDF | Download SDF |
Canonical SMILES | CC1COC2(O1)CCN(CC2)C3=NC(=O)C4=CC(=CC(=C4S3)[N+](=O)[O-])C(F)(F)F |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Description | BTZ043 racemate is an inhibitor of decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1). | |||||
Targets | DprE1 | |||||
IC50 |
Quality Control & MSDS
- View current batch:
Chemical structure

Related Biological Data

Related Biological Data
