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BTZ043 Racemate

Catalog No. T6425 CAS 957217-65-1

Synonyms: BTZ044, BTZ10526038, Benzothiazinone 10526038

BTZ043 Racemate (Benzothiazinone 10526038) is a decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1) inhibitor, used as a new antimycobacterial agent.

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BTZ043 Racemate, CAS 957217-65-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 183.00
50 mg	In stock	$ 322.00
100 mg	In stock	$ 538.00
1 mL * 10 mM (in DMSO)	In stock	$ 79.00

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Purity: 99.516%

Purity: 98.47%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	BTZ043 Racemate (Benzothiazinone 10526038) is a decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1) inhibitor, used as a new antimycobacterial agent.
In vitro	By targeting decaprenylphosphoryl-β-D-ribose 2'-epimerase, BTZ043 abolishes the formation of decaprenylphosphoryl arabinose, leading to cell lysis and death of Mycobacterium tuberculosis. BTZ043 displays similar activity against all clinical isolates of M. tuberculosis, including multidrug-resistant and extensively drug-resistant strains. BTZ043 displays significant activity against M. tuberculosis H37Rv and Mycobacterium smegmatis with MIC of 1 ng/mL (2.3 nM) and 4 ng/mL (9.2 nM), respectively, which is more potent than those of the existing tuberculosis (TB) drugs isoniazid (INH) and ethambutol (EMB) with MIC of 0.02-0.2 μg/mL and 1-5 μg/mL, respectively. BTZ043 is less effective in two different model systems (auxotrophy and starvation) involving metabolically inert M. tuberculosis, indicating that BTZ043 blocks a step in active metabolism similar to isoniazid (INH). BTZ043 treatment in M. smegmatis cells decreases the growth rate rapidly followed by a swelling of the poles and lysis of the cells after a few hours, which is similar but delayed in M. tuberculosis. [1] BTZ043 (1/4 MIC 0.375 ng/mL) in combination with TMC207 (1/4 MIC 20 ng/mL) has a stronger cidal effect on M. tuberculosis but not BTZ-resistant M. tuberculosis mutant than TMC207 alone at a concentration of 80 ng/mL. [2]
In vivo	In a mouse model of chronic tuberculosis, administration of BTZ043 at 37.5 mg/kg or 300 mg/kg for 4 weeks reduces the bacterial burden in the lungs and spleens by 1 and 2 logs, respectively. [1]

Synonyms	BTZ044, BTZ10526038, Benzothiazinone 10526038
Molecular Weight	431.39
Formula	C17H16F3N3O5S
CAS No.	957217-65-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 21 mg/mL (48.7 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Makarov V, et al. Science, 2009, 324(5928), 801-804. 2. Lechartier B, et al. Antimicrob Agents Chemother, 2012.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library Clinical Compound Library Preclinical Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Anti-Bacterial Compound Library Antibiotics Library Anti-Infection Compound Library Bioactive Compound Library

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Keywords

BTZ043 Racemate 957217-65-1 Microbiology/Virology Others Antibacterial DprE1 Benzothiazinone10526038 inhibit Benzothiazinone-10526038 BTZ-044 BTZ044 Inhibitor BTZ-043 Racemate BTZ-043 BTZ-10526038 BTZ043 BTZ 043 tuberculosis BTZ10526038 Benzothiazinone 10526038 BTZ 10526038 BTZ 044 Bacterial inhibitor

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