Name: BTZ043 Racemate
Price: 292.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    MIC: 1 ng/ml (2.3 nM) for M. tuberculosis H37Rv and 4 ng/ml (9.2 nM) for Mycobacterium smegmatisThe 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.
- Properties
  - Alternative Name
    
    2-(3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one
    
    CAS Number
    
    957217-65-1
    
    Molecular Formula
    
    C17H16F3N3O5S
    
    Molecular Weight
    
    431.39
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥10.4 mg/mL in DMSO with gentle warming; ≥3.27 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 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.

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