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GSK-729

Chemical Structure : GSK-729

CAS No.: 1260243-45-5

GSK-729 (GSK 729;GSK729)

Catalog No.: PC-61004Not For Human Use, Lab Use Only.

A potent, small molecule inhibitor of Mycobacterium tuberculosis enoyl-coenzyme A (CoA) hydratase EchA6 with IC50 of 1.8 uM, but not the MmpL3.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A potent, small molecule inhibitor of Mycobacterium tuberculosis enoyl-coenzyme A (CoA) hydratase EchA6 with IC50 of 1.8 uM, but not the MmpL3; selectively pulls down EchA6 in a stereospecific manner in M. bovis BCG extracts, competes with CoA-binding, suppresses mycolic acid synthesis, and are bactericidal in mouse model of chronic tuberculosis infection.

Physicochemical Properties

M.Wt 339.318
Formula C16H16F3N3O2
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

(5R,7S)-5-(4-ethylphenyl)-7-(trifluoromethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxylic acid

References

1. Cox JA, et al. Nat Microbiol. 2016 Jan 18;1:15006.

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