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TXA6101

Cat. No. M21096
TXA6101  Structure
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Biological Activity

TXA6101 is a filamentous temperature-sensitive mutant Z (FtsZ) protein inhibitor. TXA6101 has an antibacterial activity MIC value of 1 μg/mL against MRSA isolates expressing either G193D or G196S mutant FtsZ, retaining significant activity against the TXA707-resistant FtsZ mutant. It is being developed for use against Gram-negative bacteria.

Chemical Information
Molecular Weight 477.18
Formula C18H10BrF5N2O3
CAS Number 1459695-66-9
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jesus D Rosado-Lugo, et al. J Antibiot (Tokyo). Evaluation of 2,6-difluoro-3-(oxazol-2-ylmethoxy)benzamide chemotypes as Gram-negative FtsZ inhibitors

[2] Junso Fujita, et al. ACS Chem Biol. Structural Flexibility of an Inhibitor Overcomes Drug Resistance Mutations in Staphylococcus aureus FtsZ

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  Catalog
Abmole Inhibitor Catalog




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