Macozinone

SKU: orb1304034

Description

Macozinone (PBTZ169) is a potent small molecule inhibitor of the Mycobacterium tuberculosis enzyme DprE1, demonstrating superior inhibitory activity compared to BTZ043. It serves as a key research tool for investigating tuberculosis drug mechanisms and has shown efficacy in both in vitro and in vivo preclinical studies.

Research Area

Infectious Disease & Virology

Key Properties

• CAS Number: 1377239-83-2
• MW: 456.48
• Purity: >99.99% (May vary between batches)
• Formula: C₂₀H₂₃F₃N₄O₃S
• SMILES: [O-][N+](=O)c1cc(cc2c1sc(nc2=O)N1CCN(CC2CCCCC2)CC1)C(F)(F)F
• Target: DprE1,Antibacterial,Antibiotic
• Solubility: DMSO:4.57 mg/mL (10.01 mM)

Bioactivity

• In Vivo:
  PBTZ169 can be suspend in 0.25% hydroxy-propylmethyl-cellulose. The administertration for PBTZ169 is 100 mg/kg by gavage. The MIC50 and MIC90 values were 0.0075 and 0.030 μg/mL, respectively. The MIC for PBTZ169 for N. brasiliensis HUJEG-1 was 0.0037 μg/mL. PBTZ169 has improved potency, safety and efficacy in zebrafish and mouse models of tuberculosis (TB).
• In Vitro:
  PBTZ169, inhibit decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1) and display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

tuberculosis, antituberculosis, Bacterial, bactericidal, benzothiazinone, covalent, DprE1, inhibit, Inhibitor, Macozinone, PBTZ 169, PBTZ169, PBTZ-169

Compound Identifiers

PubChem CID

57331386