PBTZ-169, also known as macozinone, is a new drug candidate that inhibits decaprenyl-phosphoribose-epimerase (DprE1), an essential enzyme involved in the cell wall biosynthesis of Corynebacterineae. The MIC values of PBTZ-169 ranged from 0.03 μg/mL to 0.0037 μg/mL. The MIC50 and MIC90 values of PBTZ-169 were 0.0075 and 0.030 μg/mL, respectively. The MIC for PBTZ-169 for N. brasiliensis HUJEG-1 was 0.0037 μg/mL. The MICs of SXT, DA-7218, and BTZ043 for this strain were 9.5/0.5, 8, and 0.125 μg/mL, respectively.
CAS Number: 1377239-83-2
Molecular Weight: 456.48
Chemical Name: 2-(4-(cyclohexylmethyl)piperazin-1-yl)-8-nitro-6-(trifluoromethyl)-4H-benzo[e][1,3]thiazin-4-one
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: 5 mg/mL(10.95 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
PBTZ-169, inhibit decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1) and display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro.
PBTZ-169 can be suspend in 0.25% hydroxy-propylmethyl-cellulose. The administertration for PBTZ-169 is 100 mg/kg by gavage. The MIC50 and MIC90 values were 0.0075 and 0.030 μg/mL, respectively. The MIC for PBTZ-169 for N. brasiliensis HUJEG-1 was 0.0037 μg/mL. PBTZ-169 has improved potency, safety and efficacy in zebrafish and mouse models of tuberculosis (TB).
- Makarov V et al. The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 from Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2015 Aug;59(8):4446-52.
- González-Martínez NA et al. In Vivo Activity of the Benzothiazinones PBTZ169 and BTZ043 against Nocardia brasiliensis. PLoS Negl Trop Dis. 2015 Oct 16;9(10):e0004022.
- Makarov V et al. Towards a new combination therapy for tuberculosis with next generation benzothiazinones.EMBO Mol Med. 2014 Mar;6(3):372-83.
Products are for research use only. Not for human use.
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