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VXc-486

Chemical Structure : VXc-486

CAS No.: 1384984-18-2

VXc-486 (VXc486)

Catalog No.: PC-35267Not For Human Use, Lab Use Only.

VXc-486 (VXc486) is a novel inhibitor of gyrase B, potently inhibits multiple drug-sensitive isolates and drug-resistant isolates of Mycobacterium tuberculosis in vitro with MICs of 0.03-0.30 μg/ml and 0.08-5.48 μg/ml, respectively.

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Biological Activity

VXc-486 (VXc486) is a novel inhibitor of gyrase B, potently inhibits multiple drug-sensitive isolates and drug-resistant isolates of Mycobacterium tuberculosis in vitro with MICs of 0.03-0.30 μg/ml and 0.08-5.48 μg/ml, respectively; VXc-486 is active against drug-resistant isolates, has bactericidal activity, and kills intracellular and dormant M. tuberculosis bacteria in a low-oxygen environment; inhibits the growth of multiple strains of Mycobacterium abscessus, Mycobacterium avium complex, and Mycobacterium kansasii (MICs=0.1-2.0 μg/ml), as well as several strains of Nocardia spp. (MICs=0.1-1.0 μg/ml); reduces mycobacterial burdens in lungs of infected mice in vivo, sterilizes M. tuberculosis infection when combined with rifapentine-pyrazinamide and bedaquiline-pyrazinamide.

Physicochemical Properties

M.Wt 428.468
Formula C21H25FN6O3
Appearance Solid
CAS No.
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/SMILES

N-Ethyl-N'-[6-fluoro-5-[2-(1-hydroxy-1-methylethyl)-5-pyrimidinyl]-7-[(2R)-tetrahydro-2-furanyl]-1H-benzimidazol-2-yl]urea

References

1. Locher CP, et al. Antimicrob Agents Chemother. 2015 Mar;59(3):1455-65.

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