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Chemical Structure| 957217-65-1 Chemical Structure| 957217-65-1

Structure of BTZ043 Racemate
CAS No.: 957217-65-1

Chemical Structure| 957217-65-1

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BTZ043 racemate is a decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1) inhibitor acting as an antimycobacterial agent that kill Mycobacterium tuberculosis.

Synonyms: BTZ10526038; Benzothiazinone 10526038

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Product Details of BTZ043 Racemate

CAS No. :957217-65-1
Formula : C17H16F3N3O5S
M.W : 431.39
SMILES Code : O=C1N=C(N(CC2)CCC32OCC(C)O3)SC4=C([N+]([O-])=O)C=C(C(F)(F)F)C=C14
Synonyms :
BTZ10526038; Benzothiazinone 10526038
MDL No. :MFCD22420808

Safety of BTZ043 Racemate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
THP-1 77 μg/ml (TD50) 3 days Evaluate cytotoxicity, showing low cytotoxicity Antimicrob Agents Chemother. 2015 Aug;59(8):4446-52.
A549 34 μg/ml (TD50) 3 days Evaluate cytotoxicity, showing low cytotoxicity Antimicrob Agents Chemother. 2015 Aug;59(8):4446-52.
Huh7 16 μg/ml (TD50) 3 days Evaluate cytotoxicity, showing low cytotoxicity Antimicrob Agents Chemother. 2015 Aug;59(8):4446-52.
HepG2 19 μg/ml (TD50) 3 days Evaluate cytotoxicity, showing low cytotoxicity Antimicrob Agents Chemother. 2015 Aug;59(8):4446-52.
Non-replicating Mtb in caseum 512 µM 7 days To evaluate the activity of BTZ-043 against non-replicating Mtb, results showed limited activity in caseum. Antimicrob Agents Chemother. 2023 Nov 15;67(11):e0059723.
Mycobacterium smegmatis 4 ng/ml (9.2 nM) A few hours Observe the growth inhibition and cell lysis effect of BTZ043 on M. smegmatis Science. 2009 May 8;324(5928):801-4.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C3HeB/FeJ mice Tuberculosis infection model Oral 50, 100, 200 mg/kg 5 days per week for 8 weeks To evaluate the efficacy of BTZ-043 in a tuberculosis infection model, results showed significant reductions in lung and spleen bacterial burdens. Antimicrob Agents Chemother. 2023 Nov 15;67(11):e0059723.
Mice (BALB/c and IL-13 transgenic mice) Tuberculosis model (BALB/c mice and IL-13 transgenic mice) Oral gavage 50, 100, 250, 500, 1000 mg/kg/day (BALB/c mice); 250 mg/kg/day (IL-13 transgenic mice) 5 days per week for 4, 6, or 8 weeks (BALB/c mice); 10 consecutive days (IL-13 transgenic mice) To evaluate the antituberculosis activity of BTZ-043 in standard and advanced mouse models. Results showed that BTZ-043 exhibited dose- and time-dependent bactericidal activity in BALB/c mice and effectively reduced bacterial burden in both pulmonary and necrotic granulomas in IL-13 transgenic mice. Nat Commun. 2025 Jan 18;16(1):826

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.59mL

2.32mL

1.16mL

23.18mL

4.64mL

2.32mL

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