Chemical Structure : DDD02049209
CAS No.:
2973324-63-7
DDD02049209
Catalog No.: PC-25240Not For Human Use, Lab Use Only.
DDD02049209 is a potent, specific inhibitor of M. tuberculosis lysyl-tRNA synthetase (LysRS) with IC50 of 0.05 uM, inhibits M. tuberculosis phenotypic growth in culture (MIC) with 0.08 uM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
DDD02049209 is a potent, specific inhibitor of M. tuberculosis lysyl-tRNA synthetase (LysRS) with IC50 of 0.05 uM, inhibits M. tuberculosis phenotypic growth in culture (MIC) with 0.08 uM.
DDD02049209 displays exquisite selectivity (>100-fold) over the human counterpart, at both an enzyme (KARS1, IC50 > 100 μM; and cellular level (HepG2 IC50 > 100 μM).
DDD02049209 demonstrates good efficacy, achieving a >3 log10 reduction in colony forming units (CFU) with an ED99 (dose that causes a 2 Log10 reduction in CFU with respect to untreated mice) of 49 and 12 mg/kg respectively in murine models of M. tuberculosis infection, achieved a clear reduction in lung CFU, with a maximum effect of 2.4 log10 reductions and an ED99 of 94 mg/kg.
Physicochemical Properties
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M.Wt
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328.32
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Formula
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C14H18F2N4O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-amino-6-((1S,7S)-2,2-difluoro-7-hydroxycycloheptyl)-4-methoxy-6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidin-5-one
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References
1. Green SR, et al. Nat Commun. 2022 Oct 11;13(1):5992.
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