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Macozinone

Chemical Structure : Macozinone

CAS No.: 1377239-83-2

Macozinone (PBTZ169;PBTZ-169)

Catalog No.: PC-61388Not For Human Use, Lab Use Only.

Macozinone (PBTZ-169, PBTZ169) is a potent, second-generation antituberculosis agent that inhibits DprE1 and displays nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro.

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Biological Activity

Macozinone (PBTZ-169, PBTZ169) is a potent, second-generation antituberculosis agent that inhibits DprE1 and displays nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro; PBTZ169 is less cytotoxic than BTZ043 and shows significantly better efficacy at lower concentrations in the murine model of chronic TB, inhibits DprE1 more efficiently than BTZ043.

Bacterial Infection

Phase 2 Clinical

Physicochemical Properties

M.Wt 456.484
Formula C20H23F3N4O3S
CAS No. 1377239-83-2
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name

2-[4-(cyclohexylmethyl)piperazin-1-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one

References

1. Makarov V, et al. EMBO Mol Med. 2014 Mar;6(3):372-83.

2. Makarov V, et al. Antimicrob Agents Chemother. 2015 Aug;59(8):4446-52.

3. González-Martínez NA, et al. PLoS Negl Trop Dis. 2015 Oct 16;9(10):e0004022.

4. Lechartier B, et al. Antimicrob Agents Chemother. 2015 Aug;59(8):4457-63.

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